@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 {45366,
	title = {Synthesis and anticancer activity of conformationally constrained Smac mimetics containing pseudo beta turns},
	journal = {Tetrahedron Letters },
	volume = {59},
	year = {2018},
	month = {SEP},
	pages = {3473-3476},
	type = {Article},
	abstract = {Herein, we report synthesis and in vitro anticancer activity of conformationally constrained Smac mimetics containing reverse turn inducing motifs "Ant-Pro" and "sAnt-Pro". The synthesis of Smac analogs with diverse hydrophobic groups at the C-terminus was carried out using solution phase peptide synthesis. The synthesis of Ant-Pro containing analogs 3a-j was carried out by ring opening of benzoxazinones 7a-c, whereas, their sulfonamide counterparts 4a-h were synthesized by using routine acid-amine coupling reaction. In vitro anticancer studies against breast cancer cell line MDA-MB-231 revealed that some of the new analogs had better anticancer activity than the standard AVPI Smac tetrapeptide. (C) 2018 Published by Elsevier Ltd.},
	doi = {10.1016/j.tetlet.2018.08.016},
	author = {Baravkar, Sachin B. and Wagh, Mahendra A. and Paul, Debasish and Santra, Manas and Sanjayan, Gangadhar J.}
}
