Design and synthesis of pyrazole–pyrazoline hybrids as cancer‐associated selective COX‐2 inhibitors

In continuation of our previous work on cancer and inflammation, 15 novel pyrazole–pyrazoline hybrids ( WSPP1 – 15 ) were synthesized and fully characterized. The formation of the pyrazoline ring was confirmed by the appearance of three doublets of doublets in ¹H nuclear magnetic resonance spectra exhibiting an AMX pattern for three protons (H_A, H_M, and H_X) of the pyrazoline ring. All the synthesized compounds were screened for their in vitro anticancer activity against five cell lines, that is, MCF‐7, A549, SiHa, COLO205, and HepG2 cells, using the MTT growth inhibition assay. 5‐Fluorouracil was taken as the positive control in the study. It was observed that, among them, WSPP11 was found to be active against A549, SiHa, COLO205, and HepG2 cells, with IC₅₀ values of 4.94, 4.54, 4.86, and 2.09 µM. All the derivatives were also evaluated for their cytotoxicity against HaCaT cells. WSPP11 was also found to be nontoxic against normal cells (cell line HaCaT), with an IC₅₀ value of more than 50 µM. The derivatives were also evaluated for their in vitro anti‐inflammatory activity by the protein (egg albumin) denaturation assay and the red blood cell membrane stabilizing assay, using diclofenac sodium and celecoxib as standard. Compounds that showed significant anticancer and anti‐inflammatory activities were further studied for COX‐2 inhibition. The manifestation of a higher COX‐2 selectivity index of WSPP11 as compared with other derivatives and an in vitro anticancer activity against four cell lines further established that compounds that were more selective toward COX‐2 also exhibited a better spectrum of activity against various cancer cell lines.     

Novel menadione hybrids: Synthesis,anticancer activity,and cell‐based studies

A series of novel menadione‐based triazole hybrids were designed and synthesized by employing copper‐catalyzed azide‐alkyne cycloaddition (CuAAC). All the synthesized hybrids were characterized by their spectral data (¹H NMR, ¹³C NMR, IR, and HRMS). The synthesized compounds were evaluated for their anticancer activity against five selected cancer cell lines including lung (A549), prostate (DU‐145), cervical (Hela), breast (MCF‐7), and mouse melanoma (B‐16) using MTT assay. The screening results showed that majority of the synthesized compounds displayed significant anticancer activity. Among the tested compounds, the triazoles 5 and 6 exhibited potent activity against all cell lines. In particular, compound 6 showed higher potency than the standard tamoxifen and parent menadione against MCF‐7 cell line. Flow cytometric analysis revealed that compound 6 arrested cell cycle at G0/G1 phase and induced apoptotic cell death which was further confirmed by Hoechst staining, measurement of mitochondrial membrane potential (ΔΨm) and Annexin‐V‐FITC assay. Thus, compound 6 can be considered as lead molecule for further development as potent anticancer therapeutic agent.     

Design,synthesis, and cytotoxic evaluation of novel furo[2,3‐b]quinoline derivatives

A number of novel furo[2,3‐b]quinoline derivatives were designed and synthesized by introducing benzyl ether, benzoate, and benzenesulfonate to 6‐position of furo[2,3‐b]quinoline and their chemical structures were confirmed by ESI‐MS, ¹H NMR, and ¹³C NMR spectra. All target compounds were evaluated in vitro against four human cancer cell lines (HCT‐116, MCF‐7, U2OS, and A549) by MTT method. Cytotoxic assay showed that compounds 8a , 8e , 10a , 10b, and 10c exhibited more potent cytotoxicities compared to 2‐bromine‐6‐hydroxy‐furo‐[2,3‐b]quinoline ( 7 ). Compound 10c exhibited higher antiproliferative activity (IC₅₀ values ranging from 4.32 to 24.96 μm ) against four human cancer cell lines (HCT‐116, MCF‐7, U2OS, and A549) and weak cytotoxicity on normal cell HL‐7702, which suggested that 10c might be an ideal anticancer candidate. Compounds 8a , 10a , 10b showed good selectivities to MCF‐7 and HCT‐116, which could be considered as ideal selective candidates for further study. The SARs showed that the introduction of the benzyl ether and benzenesulfonate could significantly improve cytotoxicities, while the benzoate failed to enhance potency obviously.     

Synthesis and biological evaluation of novel benzo[c]acridine‐diones as potential anticancer agents and tubulin polymerization inhibitors

A new series of novel benzo[c]acridine‐diones possessing pharmacophoric elements of antitubulins with central dihydropyridine bridge were designed and synthesized as potential anticancer agents and tubulin polymerization inhibitors. The cytotoxic activity of the synthesized compounds was evaluated against eight cancer cell lines including MCF‐7, A2780, HeLa, HepG2, DU145, A549, PC3, and LNCAP cancer cells and normal cells human umbilical vein endothelial cell (HUVEC) through 3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5‐diphenyl tetrazolium bromide (MTT) assay, wherein β‐lapachone and combretastatin A‐4 were used as positive controls. Some of our compounds ( 4c and 4g ) showed significant cytotoxic activity on cancer cells with IC₅₀ values in the range of 5.23–24.32 μM. None of the synthesized compounds showed significant cytotoxicity on normal HUVEC cells. Among all investigated derivatives, compound 4g showed promising greater antiproliferative activity against all tested cancer cells with the highest sensitivity observed for the PC3 cell line. Results from the flow cytometry analysis of PC3 and MCF‐7 cancer cells treated with 4g showed an induced cell‐cycle arrest at G2/M, and therefore induced apoptosis which occurred at low concentration of test compound, whereas annexin V‐FITC/propidium iodide staining assay in the aforementioned cancer cell lines treated with 4g showed that 4g can cause necrosis in PC3 and MCF‐7 cancer cells at higher concentration. Compound 4g proved to be an inhibitor of tubulin polymerization in a mode similar to that of colchicine and in a dose‐dependent manner. Molecular docking studies of 4g into the colchicine‐binding site of tubulin exhibited a possible mode of interaction between this compound and tubulin.     

New pyrimidinone and fused pyrimidinone derivatives as potential anticancer chemotherapeutics

A series of novel substituted pyrimidinones and fused pyrimidinones (compounds 3 – 18 ) were synthesized starting with oxiranylmethanone 2 . The in vitro cytotoxicity against a human breast adenocarcinoma (MCF‐7) cell line was investigated and most of the tested compounds showed potent cytotoxic activity against the MCF‐7 cell line comparable to the activity of the commonly used anticancer drug cisplatin. Treatment of MCF‐7 cells with increasing doses (2, 5, 10, and 20 µg/mL) of the tested compounds revealed that the activity of superoxide dismutase and the level of hydrogen peroxide were significantly increased, while the activities of catalase and glutathione peroxidase and the levels of reduced glutathione were significantly lowered compared with control MCF‐7 cells. In general, derivatives 11 and 16 revealed the highest anticancer activity among the tested compounds.     

Synthesis and Biological Evaluation of Some 1,2‐Disubstituted Benzimidazole Derivatives as New Potential Anticancer Agents

The synthesis of some new 1‐(2‐aryl‐2‐oxoethyl)‐2‐[(morpholine‐4‐yl)thioxomethyl]benzimidazole derivatives and investigation of their anticancer activities were the aims of this work. 2‐(Chloromethyl)benzimidazole compound was reacted with sulfur and morpholine via Willgerodt–Kindler reaction to give 2‐[(morpholine‐4‐yl)thioxomethyl]benzimidazole. Then, the obtained compound was reacted with appropriate α‐bromoacetophenone derivatives in the presence of potassium carbonate to give the final products. Structure elucidation of the final compounds was achieved by FT‐IR, ¹H NMR spectroscopy and MS spectrometry. The anticancer activities of the final compounds were evaluated by MTT assay, BrdU method, and flow cytometric analysis on C6, MCF‐7, and A549 tumor cells. Most of the synthesized compounds exhibited considerable selectivity against the MCF‐7 and C6 cell lines.     

Reprofiling of full‐length phosphonated carbocyclic 2′‐oxa‐3′‐aza‐nucleosides toward antiproliferative agents: Synthesis,antiproliferative activity,and molecular docking study

A series of phosphonated carbocyclic 2 ′ ‐oxa‐3 ′ ‐aza‐nucleosides were synthesized via 1,3 dipolar cycloaddition and evaluated for their in vitro antiproliferative activity against the growth of cancer cell lines (MCF‐7, A2780, HCT116) and normal non‐transformed fibroblast (MRC5) using MTT assay. Synthesized compounds exhibited antiproliferative activity in the micromolar range. Compounds 11b showed the highest activity against MCF‐7 cells (IC₅₀ of 0.2344 μm ). Cell cycle analysis was performed for compound 11b on MCF7 cells showing arrest of cells in the S phase. Molecular docking of synthesized compounds confirmed high affinity of these compounds to two different receptors for anticancer nucleosides on dCK, namely the 1P5Z and 2ZIA, showing scores higher than the cognate ligand for all tested compounds. All synthesized compounds were evaluated according to the Lipinski, Veber, and Opera rules, and all of them passed the evaluation showing excellent features, superior to reference drugs. In addition, ADME for all the synthesized compounds was predicted through a theoretical kinetic study using the discovery studio 3.1 software.     

Design,synthesis, biological evaluations,molecular docking,and in vivo studies of novel phthalimide analogs

A series of novel phthalimide analogs containing an indole or brominated indole moiety were synthesized and their antimicrobial activity was evaluated. Compound 8 showed a broad spectrum activity, revealing 53–67% of erythromycin activity on the tested bacteria and 60–70% of miconazole activity on the tested fungi. Anticancer activity was evaluated on the cell lines HepG2, MCF‐7, A549, H1299, and Caco2. The results revealed that the new phthalimide analog 8 has broad‐spectrum anticancer activity toward all the tested cancer cell lines, followed by compound 11 , which showed good activity toward all the tested cell lines except for MCF‐7. The ability of the promising analogs 5 , 8 , and 11 to bind to topoisomerase II DNA gyrase was investigated. Caspase‐3 activation and Bcl‐2 assay of the best active derivatives 8 , 11 in addition to compound 5 were evaluated. The antifibrotic activity was studied in an in vivo model and the histopathological studies revealed that treatment with the new compound 8 improved the fibrotic liver tissues to normality.

     

Novel Thiophenes,Thienopyrimidines, and Triazolothienopyrimidines for the Evaluation of Anticancer and Augmentation Effects of γ‐Radiation

New derivatives of thiophenes 2 , 12 , iminoaminothieno[2,3‐d]pyrimidines 3 , 5 , and 6 , triazolothieno[2,3‐d]pyrimidines 8–11 , pyrazolo‐ and triazinothieno[2,3‐d]pyrimidines 4 , 7 , respectively, have been prepared by different synthetic procedures. Structure elucidation of the newly synthesized compounds was carried out via elemental analyses and spectral data. The antitumor activity of compounds 2 , 3 , and 9–12 was evaluated against in‐vitro cell lines (HEPG‐2 and MCF‐7). Compounds 2 , 3 , 10 , 11 , and 12 showed significant in‐vitro cytotoxic activity against hepatocellular carcinoma (HEPG‐2) compared to the reference drug Doxorubicin. Compound 2 showed significant in‐vitro cytotoxic activity against breast cancer (MCF‐7) cells compared to the reference drug Doxorubicin. The augmenting effect of γ‐radiation was assessed; here, compounds 2 , 3 , 10 , and 11 showed the most potent in‐vitro anticancer activity.     

Design,synthesis, and antitumor evaluation of quinoline‐imidazole derivatives

A series of compounds bearing quinoline‐imidazole ( 8a–e , 9a–e , 10a–e , 11a–e , and 12a–e ) not reported previously were designed and synthesized. The target compounds were evaluated for antitumor activity against A549, PC‐3, HepG2, and MCF‐7 cells by the MTT method, with NVP‐BEZ235 being the positive control. Most compounds showed moderate activity and compound 12a showed the best activity against HepG2, A549, and PC‐3 cells, with half‐maximal inhibitory concentration (IC₅₀) values of 2.42 ± 1.02 µM, 6.29 ± 0.99 µM, and 5.11 ± 1.00 µM, respectively, which was equal to NVP‐BEZ235 (0.54 ± 0.13 µM, 0.36 ± 0.06 µM, 0.20 ± 0.01 µM). Besides, the IC₅₀ value of 12a against the cell line WI‐38 (human fetal lung fibroblasts) was 32.8 ± 1.23 µM, indicating that the target compounds were selective for cancer cells. So, 11a and 12a were evaluated against PI3Kα and mTOR to find out if the compounds acted through the PI3K‐Akt‐mTOR signal transduction pathway. The inhibition ratios to PI3Kα and mTOR were slightly lower than that of NVP‐BEZ235, suggesting there may be some other mechanisms of action. The structure–activity relationships and docking study of 11a and 12a revealed that the latter was superior. Moreover, the target compounds showed better in vitro anticancer activity when the C‐6 of the quinoline ring was replaced by a bromine atom.

     

Design,synthesis, and molecular docking studies of novel quinoxaline derivatives as anticancer agents

As lung cancer was placed foremost part among other types of cancer in terms of mortality. Recent researches are widely focused on developing multi-targeted and site-specific targeted drug designs. In the present study, we designed and developed a series of quinoxaline pharmacophore derivatives as active EGFR inhibitors for the treatment of non-small cell lung cancer. The compounds were synthesized through a condensation reaction between hexane-3,4-dione and methyl 3,4-diaminobenzoate as a first step. Their structures were confirmed by ¹H-NMR, ¹³C-NMR, and HRMS spectroscopic methods. Cytotoxicity (MTT) were applied to determine anticancer activity of the compounds against breast (MCF7), fibroblast (NIH3 T3), and lung (A549) cell lines as EGFR inhibitors. Doxorubicin was used as a reference agent, compound 4i exhibited a significant effect among other derivatives with IC₅₀ = 3.902 ± 0.098 μM value against A549 cell line. The docking study showed that the best position on EGFR receptor could be observed with 4i . From the obtained evaluations of the designed series, compound 4i was a promising agent as EGFR inhibitor for further investigation and evaluation studies in the future.     

Induction of apoptosis in lung adenocarcinoma and glioma cells by some oxadiazole derivatives

Oxadiazoles have received much attention due to their wide range of biological activities including antitumor activity. In this study, we aimed to study apoptotic effects of some 1,3,4-oxadiazole derivatives on human lung adenocarcinoma (A549) and rat glioma (C6) cell lines. The cytotoxicity of the compounds on both cell lines was determined, and the effects of these compounds on DNA synthesis were measured. Compounds 2 and 6 which exhibited significant cytotoxic activity in MTT assay were chosen for flow cytometric analyses to determine apoptotic percent of cells. These compounds also exhibited better DNA synthesis inhibition activity on cancer cells. Compound 6 carrying 2,4-dichlorophenyl substituent exhibited the highest apoptotic effect on A549 cells via the induction of Caspase 3 activity. It was suggested that compounds 2 and 6 can be identified as the most promising anticancer agents against A549 and C6 cancer cell lines.     

Design,synthesis, and cytotoxic evaluation of novel scopoletin derivatives

A series of scopoletin derivatives were designed and synthesized by introducing α‐aminoacetamide, acrylamide and β‐aminopropamide, respectively, to 3‐position of scopoletin, and their chemical structures were confirmed by ESI‐MS, IR, ¹H NMR, and ¹³C NMR spectra. All target compounds were evaluated in vitro against four human cancer cell lines (MDA‐MB‐231, MCF‐7, HepG2, and A549) by MTT method. Cytotoxic assay showed that compounds 7a , 7b , 7e , 7f , 8a , and 8e exhibited more potent cytotoxicities compared to scopoletin. Besides, we have further evaluated the growth inhibitory activities of these selected compounds against normal tissue cell lines HFL‐1. Although compound 8a showed the strongest antiproliferative activity in vitro, it exhibited strong cytotoxicity on normal cells HFL‐1, which limited its further study. Compound 7a and 7b exhibited higher antiproliferative activity against MDA‐MB‐231 and HepG2 cells and weak cytotoxicity on HFL‐1, which suggested that 7a and 7b might be ideal anticancer candidates. The SARs showed that the introduction of the acrylamide and its analogues β‐aminopropamide could significantly improve activity, while the α‐aminoacetamide failed to enhance potency obviously. Therefore, the mechanism of compound 7a and 7b is worthy of further research and the structure of compound 8a should be further optimized.     

Substituent Effects on Cytotoxic Activity,Spectroscopic Property,and DNA Binding Property of Naphthalimide Derivatives

A series of novel naphthalimide derivatives NI 1‐5 containing piperazine moieties (N‐(2‐hydroxyethyl)piperazine and 1‐piperazinepropanol) and piperidine moieties (4‐piperidinemethanol, 4‐hydroxypiperidine and 4‐piperidineethanol) have been synthesized and evaluated for their cytotoxic activity, spectroscopic property, and DNA binding behaviors. It was found that substituents at the 4‐position remarkably influence the various activities of this series of compound. Compounds NI 3‐5 modified with piperidines exhibited potent cytotoxic activities against Hela, SGC‐7901, and A549 cells with the IC₅₀ values from 0.73 μm to 6.80 μm , which are better than NI 1‐2 functionalized with piperazines. Compounds NI 1‐2 showed higher binding capacity with Ct‐DNA than compounds NI 3‐5 based on studies of UV–vis, fluorescence and CD spectra. Furthermore, compounds NI 3‐5 , as DNA intercalators, showed fluorescence enhancement upon binding with Ct‐DNA. More interestingly, fluorescence imaging studies of compound NI 4 with A549 cells showed that the fluorescence predominantly appeared in the cytoplasm. These results provided a potential application of NI 3‐5 as anticancer therapeutic and cancer cell imaging agents.     

Design,Synthesis, and In Vitro Evaluation of Novel 3, 7‐Disubstituted Coumarin Derivatives as Potent Anticancer Agents

Twenty‐seven 3, 7‐disubstituted coumarin derivatives were designed, synthesized, and evaluated in vitro as anticancer agents. Most of the compounds showed moderate‐to‐potent antiproliferative activity against K562 cells. Compounds 7b and 7d were chosen to evaluate the concentration of 50% growth inhibition (GI₅₀) against SN12C, OVCAR, BxPC‐3, KATO‐III, T24, SNU‐1, WiDr, HeLa, K562, and AGS cell lines. The most potent compound 7d was selected for further cell cycle arrest assay in the AGS cell line. The in vitro data indicated that methylation of benzimidazole moiety at the 3‐position of coumarin exhibited significant enhancement of anticancer activity. This study should provide important information for further modification and optimization of coumarin derivatives as anticancer agents.     

Benzoxazole/benzothiazole‐derived VEGFR‐2 inhibitors: Design,synthesis, molecular docking,and anticancer evaluations

A novel series of benzoxazole/benzothiazole derivatives 4a–c – 11a–e were designed, synthesized, and evaluated for anticancer activity against HepG2, HCT‐116, and MCF‐7 cells. HCT‐116 was the most sensitive cell line to the influence of the new derivatives. In particular, compound 4c was found to be the most potent derivative against HepG2, HCT‐116, and MCF‐7 cells, with IC₅₀ values = 9.45 ± 0.8, 5.76 ± 0.4, and 7.36 ± 0.5 µM, respectively. Compounds 4b, 9f , and 9c showed the highest anticancer activities against HepG2 cells with IC₅₀ values of 9.97 ± 0.8, 9.99 ± 0.8, and 11.02 ± 1.0 µM, respectively, HCT‐116 cells with IC₅₀ values of 6.99 ± 0.5, 7.44 ± 0.4, and 8.15 ± 0.8 µM, respectively, and MCF‐7 cells with IC₅₀ values of 7.89 ± 0.7, 8.24 ± 0.7, and 9.32 ± 0.7 µM, respectively, in comparison with sorafenib as reference drug with IC₅₀ values of 9.18 ± 0.6, 5.47 ± 0.3, and 7.26 ± 0.3 µM, respectively. The most active compounds 4a–c, 9b,c,e,f,h , and 11c,e were further evaluated for their VEGFR‐2 inhibition. Compounds 4c and 4b potently inhibited VEGFR‐2 at IC₅₀ values of 0.12 ± 0.01 and 0.13 ± 0.02 µM, respectively, which are nearly equipotent to the sorafenib IC₅₀ value (0.10 ± 0.02 µM). Furthermore, molecular docking studies were performed for all synthesized compounds to assess their binding pattern and affinity toward the VEGFR‐2 active site.     

Synthesis of new pyrazolo[3,4‐d]pyrimidine derivatives and evaluation of their anti‐inflammatory and anticancer activities

This study reports the synthesis of two series of new purine bioisosteres comprising a pyrazolo[3,4‐d]pyrimidine scaffold linked to piperazine moiety through different amide linkages. The newly synthesized compounds were evaluated for anticancer activity against four cell lines (MDA‐MB‐231, MCF‐7, SF‐268, B16F‐10) and cyclooxygenase (COX‐2) protein expression inhibition in lipopolysaccharide (LPS)‐activated rat monocytes. The results revealed that most of the synthesized compounds showed moderate‐to‐high cytotoxic activity against at least one cell line, with compound 10b being the most active against all used cell lines (IC₅₀ values 5.5–11 μg/ml) comparable to cisplatin. In addition, six of these compounds ( 7b, 10a–d, and 12c ) demonstrated inhibition of LPS‐induced COX‐2 protein expression at low concentration (25 μg/ml) as compared to the control non‐stimulated cells and showed a COX‐2 selectivity index range comparable to diclofenac sodium. The overall results indicate that many of these pyrazolopyrimidine derivatives possess in vitro anti‐inflammatory and anticancer activities at varying doses, and the most active compounds will be subjected to in vivo pharmacological evaluation.     

4,6-双苯基-2-氨基-3-氰基吡啶类化合物的合成及其 抗肿瘤活性研究

目的 设计合成一系列4,6-双苯基-2-氨基-3-氰基吡啶类化合物,并对其体外抗肿瘤活性进行初步评价。方法 以取代苯甲醛、取代苯乙酮、丙二腈和醋酸铵为原料,经一步反应制得目标化合物。采用MTT法,以 MX-58151 为阳性对照药,以 A549、HT-29 和 SMMC-7721为测试细胞株对目标化合物进行体外抗肿瘤活性评价。 结果与结论 合成了13 个未见报道的4,6-双苯基-2-氨基-3-氰基吡啶类化合物, 其结构经¹H-NMR、MS 和 IR 谱确证。体外活性测试结果显示,多数化合物能够在较低的浓度下抑制肿瘤细胞增殖。其中,2-氨基-6-（4-氟苯基）-4-（2,3,4-三甲氧基苯基）-3-氰基吡啶 具有显著的抗肿瘤细胞增殖活性,IC₅₀值达纳摩尔级水平,明显优于阳性对照药MX-58151。     

Apoptotic effects of some carbazole derivatives on lung carcinoma and glioma cell lines

In this study, we aimed to study the apoptotic effects of 2-[(9-ethyl-9H-carbazol-3-yl)amino]-2-oxoethyl N,N-disubstituted dithiocarbamates on A549 lung carcinoma and C6 glioma cell lines. Cytotoxicity analyses of DNA synthesis and detection of apoptosis by flow cytometry were evaluated to determine the anticancer activity of the compounds on both cell lines. Compounds 2, 5, and 7 which exhibited significant cytotoxic activity in MTT assay were chosen for flow cytometric analyses to determine the apoptotic percent of cells. These compounds also exhibited better DNA synthesis inhibition activity on cancer cells. Finally, acetylcholinesterase inhibition potentials of the compounds were measured. Compound 7 carrying 4-(2-dimethylaminoethyl)piperazin-1-yl moiety was the most active apoptotic agent against A549 and C6 cells. Apoptotic effect of this compound can be attributed to its AchE inhibition activity. Compounds 2 and 5 also showed apoptotic effects on C6 glioma cell lines. Compounds 2, 5, and 7 can be identified as the most promising anticancer agents against A549 and C6 cancer cell lines.     

Synthesis and Biological Evaluation of Some Novel Polysubstituted Pyrimidine Derivatives as Potential Antimicrobial and Anticancer Agents

Synthesis and evaluation of the antimicrobial and cytotoxic activity of two series of polysubstituted pyrimidines comprising the thioether functionality and other pharmacophores, reported to contribute to various chemotherapeutic activities are described. All newly synthesized compounds were subjected to in‐vitro antibacterial and antifungal screening. Out of the compounds tested, 18 derivatives displayed an obvious inhibitory effect on the growth of the tested Gram‐positive and Gram‐negative bacterial strains, with special effectiveness against the Gram‐positive strains. Compounds 1 , 2 , 6 , 7 , 9 , 10 , 11 , 21 , and 24 revealed remarkable broad antibacterial spectrum profiles. Among those, compounds 1 , 2 , 6 , 7 , 9 , and 24 exhibited an appreciable antifungal activity against C. albicans. Compound 2 proved to be the most active antimicrobial member identified here as it showed twice the activity of ampicillin against B. subtilis and the same activity of ampicillin against M. Luteus and P. aeruginosa together with a moderate antifungal activity. Further, eleven analogs were evaluated for their in‐vitro cytotoxic potential utilizing the standard MTT assay against a panel of three human cell lines: breast adenocarcinoma MCF7, hepatocellular carcinoma HePG2, and colon carcinoma HT29. The obtained data revealed that six of the tested compounds 1 , 3 , 7 , 12 , 13 , and 15 showed a variable degree of cytotoxic activity against the tested cell lines at both the LC₅₀ and LC₉₀ levels. Compound 7 proved to be the most active cytotoxic member in this study with special effectiveness against the colon carcinoma HT29 and breast cancer MCF7 human cell lines for LC₅₀ and LC₉₀. Thus, compounds 1 and 7 could be considered as possible dual antimicrobial‐anticancer agents.