Synthesis and antitumor activity of platinum(II) complexes containing substituted ethylenediamine ligands

Synthesis and Antitumor Activity of Enantiomerically Pure [1, 2-Diamino-1-(4-fluorophenyl) propane]dichloroplatinum(II) Complexes

“…In a first series of platinum(II) complexes with ligands such as 1,2-diamino-1,2-diphenylethanes [11,12,[23][24][25][26], 1,2-diamino-1-phenylpropane [8], 1,2-diamino-3-phenylpropanes [27], 2-picoline [28] or 1-(2-aminophenyl)isoquinolines [29], it was postulated that this kind of compounds should be more strongly bound to DNA, possibly by intercalating the aromatic rings between the DNA bases.This theory was later reconsidered [30] when it was proved that aromatic groups cause a steric hindrance during the attachment to the DNA bases. Although the precise mechanism of action of platinum(II) complexes still remains imperfectly known, two facts seem well established: (i) Platinum(II) complexes bind to DNA without dissociation of their neutral ligand [6], and (ii) fixation of the complexes induces changes in the conformation of DNA [31] and inhibits DNA polymerase which in turn inhibits DNA duplication and transcription, and finally cell replication [32,33].…”

Activity of some platinum(II/IV) complexes with O,O-n-butyl-and O,O-n-pentyl-ethylenediamine-N,N′-di-3-propanoate and halogeno ligands against HeLa and K562 cell lines and human PBMC

“…Because of its severe side-effects a need of new platinum complexes has arisen, and several new derivatives have been synthesized and antitumor activity against various tumor model systems was determined, in order to discover new drugs with improved properties [6]. Platinum(II) complexes containing ethylenediamine or its derivate have also been synthesized and tested for in vitro and in vivo activity [7][8][9][10]. The ethylenediamine and its derivate afforded different activities, depend not only of chelate but, of the labile ligands as well.…”

Chiral Primary–Secondary Diamines Catalyzed Michael–Aldol–Dehydration Reaction between Benzoylacetates and α,β‐Unsaturated Ketones: Highly Enantioselective Synthesis of Functionalized Chiral Cyclohexenones

“…HPLC analysis was carried out on WATERS equipment. Catalysts 3 a-d, [10] 3e, [15] 3 f, [16] and 3 g [17] were prepared from known procedure.…”