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A highly efficient protocol was developed for the synthesis of 3-(indoline-1-carbonyl)-N-(substituted)benzenesulfonamide compounds with excellent yields. The in vitro anticancer activity of the new 3-(indoline-1-carbonyl)-N-(substituted)benzenesulfonamide derivatives against A549 (lung cancer cell), HeLa (cervical), MCF-7 (breast cancer cell) and Du-145 (prostate cancer cell) cell lines were studied. Most of the tested compounds showed anticancer activity (IC50 values ranged between 1.98 and 9.12 µM against different cell lines).

2,3-Dihydroquinazolin-4(1H)-one derivatives (3a-p) were synthesized in excellent yields. These compounds were screened for antiproliferative activity against A549 cells and were found as potent cytotoxicity. Compounds A4, A8, A10 found to be more promising antiproliferative against the lung carcinoma A549 cells. IC50 values for compounds A4, A8 and A10 were found to be 8.6, 8.9 and 8.1 μg/L against A549 cells, respectively. KEYWORDS Ionic liquidGreen chemistry 2-Aminobenzamide Antiproliferative activity Lung carcinoma A549 cells 2,3-Dihydroquinazolin-4(1H)-one Cite this: Eur.

A series of Rhodanine derivatives were synthesized by Knoevenagel condensation. All the synthesized compounds were tested for their in vitro anticancer activity against MCF-7 and BT-474 human breast cancer cell lines. All the synthesized compounds were characterized and screened for their antimicrobial activity against the bacterial and fungal strain. Majority of the compounds showed good to moderate anticancer and antimicrobial activity. Among these compounds, one showed promising activity against gram-positive bacteria B. subtilis and S. aureus when compared with ampicillin. Some of the most potent compounds possessed selective antimicrobial activity.

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A library of 2,3‐dihydroquinazolin‐4(1H)‐one derivatives (5 a‐k) were synthesized in good yield by using 1‐Ethyl‐3‐Methylimidazolium hydrogen sulphate (10 mol %) as a catalyst and were evaluated for their anti‐biofilm, antimicrobial and cytotoxicity potential. Among the synthesized compounds, 2‐(4‐(1H‐1,2,4‐triazol‐1‐yl)phenyl)‐2,3‐dihydroquinazolin‐4(1H)‐one (5d) and 2,3‐dihydro‐2‐(2,4,6‐trimethoxyphenyl) quinazolin‐4(1H)‐one (5j) displayed better anti‐biofilm activity than fluconazole (IC50 = 40 μM) with IC50 values less than 30 μM. Compound 5d also appeared to be fungicidal against C. Albicans having MIC=33.5 μg/ml comparable with standard fluconazole (50 μg/ml). All the synthesized compounds were also evaluated for cytotoxic activity by using MTT assay against HeLa, A‐549 and MDA‐MB‐231 cell lines. The compound 5d was found to be more potent against MDA‐MB‐231 and A549 cell lines (IC50 = 11 ± 2 μM and 34±8 μM respectively) than 5‐fluorouracil (IC50 = 19 ± 3 μM and 51 ± 5 μM respectively). The compounds substituted with 6‐methyl‐4‐oxo‐4H‐chromen‐3‐yl (5a), biphenyl (5c) and 2‐hydroxy‐5‐bromophenyl (5e) were also found to be more potent against MDA‐MB‐231 cell lines (IC50 = 13 ± 3 – 14 ± 4 μM) than 5‐fluorouracil. Molecular docking simulations were also carried out using secreted aspartyl protease (SAP5), pepA enzyme of C. albicans for biofilm inhibition and EGFR tyrosine kinase for cyto‐toxicity studies. The study reveals that the compounds 5d and 5e can serve as an important lead moiety for biofilm inhibition and cyto‐toxicity against MDA‐MB‐231 and A549 cancer cell‐lines indicating their potential in the treatment of tougher fungal infections and breast and lung cancer.

An efficient, expedient, clean and environmental being synthesis of tetrahydrobenzo[b]pyran's twenty derivatives (4 a–t) has been reported via one‐pot three component condensation reaction of various benzaldehydes, dimedone and malononitrile in presence of ionic liquid [(EMIM)Ac] as a catalyst at ambient temperature in ethanol. Advantages of these reaction follow the principle of green chemistry, which are operational simplicity, shorter reaction time, and mild reaction conditions with high yield (78–98 %) products.

A series of novel fluorine containing α‐aminophosphonate derivatives (4 a–4 q) were synthesized in excellent yield and high purity. All these novel Fluorinated α‐aminophosphonate compounds were screened for antiproliferative and apoptosis activity on human non small cell lung carcinoma cells (A549) and human skin melanoma cells (SK‐MEL‐2). Compounds 4 a, 4 b, 4 c, 4 f, 4 i, 4 j and 4 m were found to be more active antiproliferative agent against A549 and SK‐MEL‐2 cells with IC50 value 0.22 to 1.25 μM. Molecular docking study related to binding affinity and binding mode analysis showed that synthesized compounds had potential to inhibit human Topoisomerase IIa enzyme system. Flow cytometric study showed some of these derivatives also induced cell apoptosis and arrest cell cycle at G1 and at G2/M phase. Overall, this study provides future perspective of lead candidate for the future anticancer drug discovery initiatives.