02195nas a2200277   4500008004100000022001400041245011700055210006900172260010600241300001400347490000700361520119800368653001501566653001901581653001201600653001401612653001201626100002201638700001901660700002401679700002201703700001801725700002301743700002801766856012301794       2013                        eng d  a0960-894X00aCorrelation of hydrogen-bonding propensity and anticancer profile of tetrazole-tethered combretastatin analogues0 aCorrelation of hydrogenbonding propensity and anticancer profile  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcAUG  a4680-46840 v233 a<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>10aColchicine10aCombretastatin10aCrystal10aTetrazole10aTubulin1 aJedhe, Ganesh, S.1 aPaul, Debasish1 aGonnade, Rajesh, G.1 aSantra, Manas, K.1 aHamel, Ernest1 aNguyen, Tam, Luong1 aSanjayan, Gangadhar, J.  uhttps://library.ncl.res.in/content/correlation-hydrogen-bonding-propensity-and-anticancer-profile-tetrazole-tethered-001419nas a2200181   4500008004100000245011300041210006900154260000800223300001400231490000700245520074500252100002500997700002301022700001901045700001801064700002801082856012701110       2018                        eng d00aSynthesis and anticancer activity of conformationally constrained Smac mimetics containing pseudo beta turns0 aSynthesis and anticancer activity of conformationally constraine  cSEP  a3473-34760 v593 aHerein, 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.1 aBaravkar, Sachin, B.1 aWagh, Mahendra, A.1 aPaul, Debasish1 aSantra, Manas1 aSanjayan, Gangadhar, J.  uhttps://library.ncl.res.in/content/synthesis-and-anticancer-activity-conformationally-constrained-smac-mimetics-containing