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41994-51-8

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Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b] isoquinoline derivatives, synthesis and biological activity
A series of linear pyrrolo[1,2-b]isoquinoline derivatives was synthesized for antitumor evaluation. The preliminary antitumor studies reveal that both bis(hydroxymethyl) and their bis(alkylcarbamate) derivatives show significant antitumor activity in inhibiting various human tumor cell growth in vitro. 1,2-Bis(hydroxymethyl)-3-methyl-5,10-dihydropyrrolo[1,2-b]isoquinoline (20a) was selected for antitumor studies in animal models. The results show that this agent can induce complete tumor remission or significant suppression in nude mice bearing human breast (MX-1) xenograft and ovarian (SK-OV-3) xenografts, respectively. Alkaline agarose gel shifting assay showed that 20a is able to cross-link with DNA. Studies on the cell cycle inhibition revealed that this agent induces cell arrest at G2/M phase. The results warrant further antitumor investigation against other human tumor growth in animal models.
Chaniyara, Ravi,Kapuriya, Naval,Dong, Huajin,Lee, Pei-Chih,Suman, Sharda,Marvania, Bhavin,Chou, Ting-Chao,Lee, Te-Chang,Kakadiya, Rajesh,Shah, Anamik,Su, Tsann-Long
experimental part
p. 275 - 286
(2011/02/27)

Retroviral protease inhibitors
The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.
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(2008/06/13)

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Chemical Properties

Appearance/Colour :white to off-white crystalline powder
Melting Point: >300 °C(lit.)
Boiling Point: 372°Cat760mmHg
Flash Point:178.8°C
Density: 1.225g/cm³
Vapor Pressure: 3.41E-06mmHg at 25°C
BRN: 3723332
PSA: 49.33000
LogP: 1.11430

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