- Synthesis and anticancer activity of new class of bisphosphonates/phosphanamidates
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Novel bis-heterocyclic bisphosphonates/phosphonamidates were synthesized utilizing the Pudovick reaction. The employment of Nb2O5 as catalyst was found to increase the yields and purity of the bisbenzoxazaphosphine derivatives (13a-h). Their anticancer activity studies in vitro, on three human tumor cell lines NCI-H460 (lung large cell), MCF-7 (breast adenocarcinoma), and SF-268 (central nervous system glioblastoma), showed that bis-[3-(3-chloro-4-fluorophenyl)-2-oxo-3,4-dihydro-2H-2λ5-benzo[e][1,3,2]oxazaphosphinin-2-yl]arylmethanes (13a-h) and [(4-chlorophenyl)-(hydroxyamidophosphinoyl)-methyl]phosphonic acid (14) exhibited significant anticancer activity.
- Kiran,Devendranath Reddy,Gunasekar,Suresh Reddy,Leon, Annette,Barbosa, Luiz C.A.
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p. 885 - 892
(2008/09/20)
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- Chlorophosphonates: Inexpensive precursors for stereodefined chloro- substituted olefins and unsymmetrical disubstituted acetylenes
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New chlorophosphonates bearing a 1,3,2-dioxaphosphorinane ring which are useful for the stereospecific synthesis of 5-chlorofurfuryl substituted olefins and chloro-substituted dienes have been obtained by an easy, inexpensive route. The utility of some of these in the synthesis of ferrocenyl- and anthracenyl-substituted unsymmetrical acetylenes has been explored. The structures of the phosphonates (OCH2CMe2CH2O)P(O)CH2(C4H2ClO) (4) and (OCH2CMe2CH2O)P(O)(CH=CHCH(Cl)Ph (7) have been determined; in addition, the stereochemistry of (5-chlorofurfuryl)CH=CH(4-ClC6H4) (13b) and 2,4- Cl2C6H3-CH=CH-CH=C(Ph)Cl (14a) is unambiguously proved by the X-ray structure determination.
- Muthiah,Praveen Kumar,Aruna Mani,Kumara Swamy
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p. 3733 - 3737
(2007/10/03)
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