01854nas a2200217   4500008004100000022001400041245017300055210006900228260007700297300001400374520092900388653002101317653001601338653001901354653004001373653001901413100001901432700002701451700002901478856012901507       2008                        eng d  a1434-193X00aSuzuki cross-coupling and intramolecular aza-michael addition reaction sequence towards the synthesis of 1,10b-epi-7-deoxypancratistatins and their cytotoxicity studies0 aSuzuki crosscoupling and intramolecular azamichael addition reac  aPO BOX 10 11 61, D-69451 WEINHEIM, GERMANYbWILEY-V C H VERLAG GMBHcDEC  a5839-58473 a<p>The development of an efficient approach to the construction of a phenanthridone is described. The convergent strategy commences with the preparation of Suzuki cross-coupling reaction precursors, arylboronic acid 12 and a-iodo enone 14, from piperonylamine (9) and (-)-D-quinic acid (10), respectively. The coupling of 12 and 19 followed by a key intramolecular aza-Michael addition produced phenanthridone 21 featuring a cis-fused B-C ring junction. The syntheses of compounds 25 and 26, both of which are C-1 and C-10b epimers of the naturally occurring potent antitumor agent 7-deoxypancratistatin (2), from 21 are elaborated in detail in this paper. The cytotoxicities of 25 and 26 were evaluated against three different cancer cell lines. Compound 26 served as a moderate growth inhibitor of THP-1 monocytic cells (GI(50) = 14.5 mu g/mL). ((C) Wiley-VCH Verlag GmbH &amp; Co. KGaA, 69451 Weinheim, Germany, 2008)</p>10aantitumor agents10aChiral pool10aCross-coupling10aIntramolecular aza-Michael addition10aPancratistatin1 aPandey, Ganesh1 aBalakrishnan, Madhesan1 aSwaroop, Pandrangi, Siva  uhttps://library.ncl.res.in/content/suzuki-cross-coupling-and-intramolecular-aza-michael-addition-reaction-sequence-towards-002518nas a2200277   4500008004100000022001400041245013400055210006900189260007500258300001400333490000700347520153500354653002101889653001501910653001201925653001901937653002601956100001601982700002101998700002102019700001802040700002002058700001702078700001702095856012802112       2015                        eng d  a0947-653900aCytostatic ruthenium(II)-platinum(II) bis(terpyridyl) anticancer complex that blocks entry into sphase by up-regulating p27(KIP1)0 aCytostatic rutheniumIIplatinumII bisterpyridyl anticancer comple  aPOSTFACH 101161, 69451 WEINHEIM, GERMANYbWILEY-V C H VERLAG GMBHcJUN  a9185-91970 v213 a<p>Cytostatic agents that interfere with specific cellular components to prevent cancer cell growth offer an attractive alternative, or complement, to traditional cytotoxic chemotherapy. Here, we describe the synthesis and characterization of a new binuclear Ru-II-Pt-II complex [Ru(tpy)(tpypma)Pt(Cl)(DMSO)](3+) (tpy=2,2:6,2-terpyridine and tpypma=4-([2,2:6,2-terpyridine]-4-yl)-N-(pyridin-2-ylmethyl)aniline), VR54, which employs the extended terpyridine tpypma ligand to link the two metal centres. In cell-free conditions, VR54 binds DNA by non-intercalative reversible mechanisms (K-b=1.3x10(5)M(-1)) and does not irreversibly bind guanosine. Cellular studies reveal that VR54 suppresses proliferation of A2780 ovarian cancer cells with no cross-resistance in the A2780CIS cisplatin-resistant cell line. Through the preparation of mononuclear Ru-II and Pt-II structural derivatives it was determined that both metal centres are required for this anti-proliferative activity. In stark contrast to cisplatin, VR54 neither activates the DNA-damage response network nor induces significant levels of cell death. Instead, VR54 is cytostatic and inhibits cell proliferation by up-regulating the cyclin-dependent kinase inhibitor p27(KIP1) and inhibiting retinoblastoma protein phosphorylation, which blocks entry into Sphase and results in G1 cell cycle arrest. Thus, VR54 inhibits cancer cell growth by a gain of function at the G1 restriction point. This is the first metal-coordination compound to demonstrate such activity.</p>10aantitumor agents10acytostatic10ap27KIP110aplatinum drugs10aruthenium terpyridine1 aRamu, Vadde1 aGill, Martin, R.1 aJarman, Paul, J.1 aTurton, David1 aThomas, Jim, A.1 aDas, Amitava1 aSmythe, Carl  uhttps://library.ncl.res.in/content/cytostatic-rutheniumii-platinumii-bisterpyridyl-anticancer-complex-blocks-entry-sphase-1