851651-86-0Relevant articles and documents
Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach
Tala, Satishkumar D.,Ou, Tai-Hsin,Lin, Yi-Wen,Tala, Kiranben S.,Chao, Shu-Hsin,Wu, Ming-Hsi,Tsai, Tung-Hu,Kakadiya, Rajesh,Suman, Sharda,Chen, Ching-Huang,Lee, Te-Chang,Su, Tsann-Long
, p. 155 - 169 (2014/03/21)
A series of new, water-soluble phenyl N-mustard-benzenealkylamide conjugates containing hydrophilic ω-dialkylaminoalkylamide or ω-cyclic aminoalkylamide moieties were synthesized via a bioisostere approach. These compounds have a broad spectrum of antitumor activity against a panel of human tumor cell lines. Of these derivatives, compound 18b effectively suppressed the growth of colon cancer (HCT-116), prostate cancer (PC3), and lung cancer (H460) xenografts. The growth of HCT-116 xenografts was almost completely suppressed when co-treated with compound 18b and 5-fluorouracil. Furthermore, compound 18b can induce DNA cross-linking and cell-cycle arrest at the G2/M phase. Early preclinical studies, including pharmacokinetics in rats, inhibition of the hERG, and 14 days of acute intravenous injection toxicity, suggest that compound 18b is a promising candidate for further preclinical studies.
Structure-based design of selective high-affinity telomeric quadruplex-binding ligands
Lombardo, Caterina Maria,Martinez, Iria Sanchez,Haider, Shozeb,Gabelica, Valerie,De Pauw, Edwin,Moses, John E.,Neidle, Stephen
supporting information; experimental part, p. 9116 - 9118 (2011/02/23)
A library of triazole-based telomeric quadruplex-selective ligands has been developed that mimic an established family of tri-substituted acridine-based ligands, using crystal structure data as a starting-point for computer-based design. Binding affinities, estimated by electrospray mass spectrometry, are in accord with the design concept.
UREYLENE DERIVATIVES
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, (2008/12/04)
The invention concerns compounds of Formula (I) or a salt, solvate or pro-drug thereof. The compounds may be used in therapy, particularly anti-cancer therapy.