@article { ISI:000322611900037,
	title = {Correlation of hydrogen-bonding propensity and anticancer profile of tetrazole-tethered combretastatin analogues},
	journal = {Bioorganic \& Medicinal Chemistry Letters},
	volume = {23},
	number = {16},
	year = {2013},
	month = {AUG},
	pages = {4680-4684},
	publisher = {PERGAMON-ELSEVIER SCIENCE LTD},
	address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND},
	abstract = {<p>A series of 1,5-disubstituted tetrazole-tethered combretastatin analogues with extended hydrogen-bond donors at the ortho-positions of the aryl A and B rings were developed and evaluated for their antitubulin and antiproliferative activity. We wanted to test whether intramolecular hydrogen-bonding used as a conformational locking element in these analogues would improve their activity. The correlation of crystal structures with the antitubulin and antiproliferative profiles of the modified analogues suggested that hydrogen-bond-mediated conformational control of the A ring is deleterious to the bioactivity. In contrast, although there was no clear evidence that intramolecular hydrogen bonding to the B ring enhanced activity, we found that increased substitution on the B ring had a positive effect on antitubulin and antiproliferative activity. Among the various analogues synthesized, compounds 5d and 5e, having hydrogen-bonding donor groups at the ortho and meta-positions on the 4-methoxy phenyl B ring, are strong inhibitors of tubulin polymerization and antiproliferative agents having IC50 value in micromolar concentrations. (C) 2013 Elsevier Ltd. All rights reserved.</p>},
	keywords = {Colchicine, Combretastatin, Crystal, Tetrazole, Tubulin},
	issn = {0960-894X},
	doi = {10.1016/j.bmcl.2013.06.004},
	author = {Jedhe, Ganesh S. and Paul, Debasish and Gonnade, Rajesh G. and Santra, Manas K. and Hamel, Ernest and Tam Luong Nguyen and Sanjayan, Gangadhar J.}
}
@article { ISI:000353205000033,
	title = {Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity},
	journal = {Bioorganic \& Medicinal Chemistry Letters},
	volume = {25},
	number = {9},
	year = {2015},
	month = {MAY},
	pages = {1982-1985},
	publisher = {PERGAMON-ELSEVIER SCIENCE LTD},
	address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND},
	abstract = {<p>We describe the design, synthesis and SAR profiling of a series of novel combretastatin-nocodazole conjugates as potential anticancer agents. The thiophene ring in the nocodazole moiety was replaced by a substituted phenyl ring from the combretastatin moiety to design novel hybrid analogues. The hydroxyl group at the ortho position in compounds 2, 3 and 4 was used as the conformationally locking tool by anticipated six-membered hydrogen bonding. The bioactivity profiles of all compounds as tubulin polymerization inhibitors and as antiproliferative agents against the A-549 human lung cancer cell line were investigated Compounds 1 and 4 showed mu M IC50 values in both assays. (C) 2015 Elsevier Ltd. All rights reserved.</p>},
	keywords = {Anticancer, Colchicine, Nocodazole, Tubulin binding},
	issn = {0960-894X},
	doi = {10.1016/j.bmcl.2015.03.019},
	author = {Kale, Sangram S. and Jedhe, Ganesh S. and Meshram, Sachin N. and Santra, Manas K. and Hamel, Ernest and Sanjayan, Gangadhar J.}
}
