@article { ISI:000261546900021,
	title = {Suzuki cross-coupling and intramolecular aza-michael addition reaction sequence towards the synthesis of 1,10b-epi-7-deoxypancratistatins and their cytotoxicity studies},
	journal = {European Journal of Organic Chemistry},
	number = {34},
	year = {2008},
	month = {DEC},
	pages = {5839-5847},
	publisher = {WILEY-V C H VERLAG GMBH},
	type = {Article},
	address = {PO BOX 10 11 61, D-69451 WEINHEIM, GERMANY},
	abstract = {<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>},
	keywords = {antitumor agents, Chiral pool, Cross-coupling, Intramolecular aza-Michael addition, Pancratistatin},
	issn = {1434-193X},
	doi = {10.1002/ejoc.200800830},
	author = {Pandey, Ganesh and Balakrishnan, Madhesan and Swaroop, Pandrangi Siva}
}
@article { ISI:000355762900032,
	title = {Cytostatic ruthenium(II)-platinum(II) bis(terpyridyl) anticancer complex that blocks entry into sphase by up-regulating p27(KIP1)},
	journal = {Chemistry-A European Journal},
	volume = {21},
	number = {25},
	year = {2015},
	month = {JUN},
	pages = {9185-9197},
	publisher = {WILEY-V C H VERLAG GMBH},
	address = {POSTFACH 101161, 69451 WEINHEIM, GERMANY},
	abstract = {<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>},
	keywords = {antitumor agents, cytostatic, p27KIP1, platinum drugs, ruthenium terpyridine},
	issn = {0947-6539},
	doi = {10.1002/chem.201500561},
	author = {Ramu, Vadde and Gill, Martin R. and Jarman, Paul J. and Turton, David and Thomas, Jim A. and Das, Amitava and Smythe, Carl}
}
