Current Organic Chemistry - Volume 18, Issue 19, 2014

Tubulin represents a potent target in cancer chemotherapy. Combretastatin is a naturally occurring well known tubulin polymerization inhibitor. Combretastatin and its analogues have been discussed in this review in detail. For better understanding, this review is subdivided as per the carbon distance between to the two aromatic rings. Under these heading, various synthetic analogues, general synthetic route, their brief SAR and structures of the most potent compound has been discussed. This article will be a good platform to guide the chemist to design and synthesize drug like molecules for tubulin polymerization inhibitory potential with optimized pharmacokinetic profile.

Pyridines and their derivatives with various functional groups possess diverse therapeutic and industrial importance. Malononitrile is a versatile reagent in organic chemistry and widely used in various multi-component reactions as a one component for the synthesis of diverse bioactive heterocycles. Malononitrile showed exceptional reactivity than other active methylene group containing compounds due to the presence of two electron withdrawing groups. In this review, we wish to report the MCRs for the synthesis of various functionalized pyridines in which one of the starting materials is malononitrile. The present review is focusing on reports from 2006- 2013.

Functionalized ionic liquids (FILs) synthesized with specific desired chemical properties have shown promising results in various areas of organic synthesis. In supported organic synthesis, FILs have become known as a new alternative to commonly used PEG and fluorous soluble supports. This review summarizes the progress of recent development in the synthesis of functionalized ionic liquids with emphasis on their applications as reagents and scavengers in organic synthesis.

An efficient tandem and domino protocol for the synthesis of chromeno-, pyrano-, and quinolino- fused spiro[pyrazolo[3,4- b]pyridine-indolines] has been developed. The present method involves one-pot pseudo five-component reaction of hydrazine hydrate and ethyl acetoacetate with isatin, malonitrile/ cyclic β-diketones and ammonium acetate/ primary aromatic amines in ethanol without using catalyst.

In the present paper, novel compounds 1-(2-(3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)-5-(pyridin-4-yl)-1,3,4-oxadiazol- 3(2H)-yl)-3-(aryl)prop-2-en-1-ones 5a-m were synthesized via cyclization of hydrazone derivative 3 with acetic anhydride and further proceeded by Claisen Schmidt reaction with different aromatic aldehydes. Synthesis of title compounds 5a-m was achieved using both conventional and microwave irradiation techniques. The yields ranged between 79-91% using microwave method and between 59-66% using conventional method. All the novel compounds 5a-m were evaluated for their in vitro antibacterial and antifungal potency against Gram-positive, Gram-negative strains of bacteria as well as fungal strains respectively and in vitro cytotoxicity study (HeLa cell lines) using MTT colorimetric assay. Among the screened compounds, 5e, 5f, 5j, 5k and 5l showed most potent antibacterial activity, while compounds 5e, 5f, 5i, 5k and 5l demonstrated excellent antifungal activity. The structure activity relationship showed that occurrence of electron donating groups witnessed substantial improvement in the antimicrobial activity. While the outcome of MTT cytotoxicity studies on HeLa cells exposed that strong antimicrobial activity of 5e, 5f and 5i-l was escorted with low cytotoxicity