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In the present investigation, novel quinolines have been synthesized and analyzed for their invitro cytotoxic activity against human colon cancer and lung cancer cells. Among the newly synthesized quinoline derivatives, 2-(3-chlorophenyl)-6,7-dimethoxyquinoline (Q6) showed considerable cytotoxic activity against human colon cancer (HCT116) and lung cancer (A549) cell lines with IC50 values of 25.5 ± 2.7 and 32 ± 4.7 μM respectively. Since these quinolines interacted with an Aurora kinase A, we carried out the molecular docking investigation and observed that this quinoline displayed inhibitory potentials. Overall, the compound Q6 was well suited to develop a newer quinolines-based anticancer medication, especially to block cell cycle arrest through Aurora kinase A inhibitors in human cancer.

One pot selective syn diacetoxylation of in situ generated cinnamic esters using PhI(OAc)2/T3P system, started from gem‑dibromomethylarenes in the presence malonoate esters/malononitrile. A broad range of substrates including both electron-deficient and electron-donating gem‑dibromomethylarenes could be efficiently elaborated by this developed methodology thereby furnishing the desired products in good to excellent yields.

An efficient methodology is reported for the regioselective C-6 arylation of protected uracil via the palladium catalyzed C H functionalization of 1-(4-methoxybenzyl)-3-methylpyrimidine-2,4(1H,3H)-dione with (hetero)aryl halides and boronic acids. Utilization of the Pd(OAc)2/Xantphos catalytic system with a stoichiometric amount of CuI and DBU as the base was vital for the success of this protocol. The methodology is facile and compatible with aryl bromides, iodides and boronic acids and hence affords broad substrate scope and diversity.

In this paper, we report the synthesis of a nano acid catalyst ZrO2–Al2O3 by using urea as a fuel and the evaluation of its catalytic efficiency in the synthesis of a series of novel substituted dihydroquinazolinones. The catalyst was found to be a highly effective solid acid catalyst, and it exhibited significant catalytic activity in converting substituted 2-aminobenzamides into corresponding 2, 3-dihydroquinazolin-4(1H)-ones under mild conditions. The optimized synthetic method is facile, rapid and efficient and may emerge as one of the best methodologies for accessing pharmaceutically useful dihydroquinazolines.

Propylphosphonic anhydride (T3P®)-DMSO mediated oxidation of alcohols to carbonyl compounds and their subsequent cyclization with aryl/hetero aryl amines and thioglycolic acid to afford 4-thiazolidinones has been reported. Synthesis of 4-thiazolidinones directly from alcohols has been carried out for the first time. Mild reaction conditions, wide functional group tolerance, ease of work-up, and good yields are the noteworthy features of this protocol.