- PYRIMIDONE DERIVATIVES AS SELECTIVE CYTOTOXIC AGENTS AGAINST HIV INFECTED CELLS
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The present disclosure is directed to pyrimidone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
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- Efficient One-Pot Synthesis of Tetrahydronaphtho[2,1-f]isoquinolines by Using Domino Pictet–Spengler/Friedel–Crafts-Type Reactions
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This study describes a facile and efficient one-pot method for the synthesis of a tetrahydronaphtho[2,1-f]isoquinoline alkaloid. An N-protected amino aldehyde biaryl substrate underwent domino Pictet–Spengler/Friedel–Crafts-type cyclization reactions to p
- Khunnawutmanotham, Nisachon,Sahakitpichan, Poolsak,Chimnoi, Nitirat,Techasakul, Supanna
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p. 6434 - 6440
(2017/12/01)
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- Synthesis and antitumor activity of feruloyl and caffeoyl derivatives This paper is dedicated to Prof. Wei-xiao Hu for his lifelong commitment to mentoring graduate students
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We developed two efficient protocols for the synthesis of feruloyl and caffeoyl derivatives from commercial vanillin and veratraldehyde. Pharmacological activities were assessed against a panel of human cancer cell lines in vitro. Most synthesized compounds demonstrated attractive cytotoxicity. Several new compounds demonstrated significant antiproliferative and cytotoxic activities against HeLa and Bewo tumor cell lines. In particular, 5-nitro caffeic adamantyl ester showed broad spectrum of tumor inhibition in 10 cell lines, and reduced tumor weight by 36.7% in vivo when administered at a dose of 40 mg kg-1.
- Chen, Hui-Zhen,Chen, You-Bao,Lv, Ya-Ping,Zeng, Fang,Zhang, Juan,Zhou, Yong-Lie,Li, Han-Bing,Chen, Li-Fei,Zhou, Bin-Jie,Gao, Jian-Rong,Xia, Chun-Nian
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supporting information
p. 4367 - 4371
(2015/02/06)
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- Synthesis and biological evaluation of ABCD ring fragments of the kibdelones
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Arylation goes platinum: The synthesis of the ABCD ring fragments of the kibdelones has been achieved through a novel PtIV-catalyzed arylation of a quinone monoketal followed by photocyclization (see scheme). Biological evaluation in the NCI 60-cell screen revealed that the kibdelone ABCD ring analogues were about 2000 times less active than kibdelones B and C, suggesting that the tetrahydroxanthone structure of the kibdelones is crucial for cytotoxicity. Copyright
- Sloman, David L.,Mitasev, Branko,Scully, Stephen S.,Beutler, John A.,Porco Jr., John A.
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p. 2511 - 2515
(2011/05/04)
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- Design, synthesis and biological evaluation of novel 4-hydroxybenzene acrylic acid derivatives
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A series of 4-hydroxybenzene acrylic acid derivatives were designed and synthesized based on the ferulic acid of natural active ingredients. The tested compound 5a, 5f and 6a have significant anti-inflammatory activity with suppression rates of 45.29%, 44.75% and 24.11%, respectively, compared with that of indomethacin, and their cardiac toxicity was not observed. The structure-function relationship shows that the p-hydroxyl group on the α-position benzene ring, particularly if acetylated, contributes to the considerable anti-inflammatory activity; that the carboxyl group on the double bond, if esterified, also contributes to the anti-inflammatory activity; that the p-methylsulfonyl group on the other benzene ring, whose introduction is due to the COX-2 selectivity, also contributes to anti-inflammatory activity surprisingly.
- Mao, Jin-Long,Ran, Xiang-Kai,Tian, Jing-Zhen,Jiao, Bo,Zhou, Hong-Lei,Chen, Li,Wang, Zhen-Guo
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scheme or table
p. 1549 - 1553
(2011/04/22)
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- Chemoselective bromodeboronation of organotrifluoroborates using tetrabutylammonium tribromide: Application in (Z)-dibromoalkene syntheses
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(Chemical Equation Presented) Tetrabutylammonlum trlbromlde (TBATB) has been found to be a unique bromodeboronatlon reagent for organotrlf luoroborates. When compared to previously reported bromodeboronatlon methods, the mild and metal-free reaction conditions tolerate a wider range of functional groups. High reglo- and chemoselectlvlty are observed In the presence of both unsaturated carbon-carbon bonds and aldehyde functional groups. An efficient synthetic route to (Z)-dlbromoalkenes from terminal alkynes has been developed using the TBATB-medlated bromodeboronatlon as a key step.
- Yao, Min-Liang,Reddy, Marepally Srinivasa,Li, Yong,Walfish, Ingrid,Blevins, David W.,Kabalka, George W.
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supporting information; experimental part
p. 700 - 703
(2010/04/02)
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- Synthesis of bastadin analogs through an SNAr coupling strategy
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The synthesis of a bastadin-5 analog was achieved in 16% overall yield (16 steps, longest linear sequence) using a strategy of intermolecular SNAr coupling to create diphenyl ether bonds and sequential amide couplings to close the ring. Noteworthy elements include assembly of all four substituted aryl rings from two simple benzaldehydes, strict regiocontrol of meta- versus para-aryl ether bonds and management of the reductively-sensitive aryl bromine substituents.
- Bailey, Karl L.,Molinski, Tadeusz F.
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p. 9657 - 9661
(2007/10/03)
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