76282-66-1Relevant academic research and scientific papers
Dienophilicity of imidazole in inverse electron demand Diels-Alder reactions. 4. Intermolecular reactions with 1,2,4-triazines
Lahue, Brian R.,Wan, Zhao-Kui,Snyder, John K.
, p. 4345 - 4354 (2003)
Intermolecular inverse electron demand cycloadditions of 2-substituted imidazoles with various 1,2,4-triazines produced both imidazo[4,5-c]pyridines (3-deazapurines) and pyrido[3,2-d]pyrimid-4-ones (8-deazapteridines). The product distribution was control
Synthesis and structure-activity relationships of TAN-1511 analogues as potent hematopoietic agents
Itoh, Fumio,Nishikimi, Yuji,Hasuoka, Atsushi,Yoshioka, Yoshio,Yukishige, Koichi,Tanida, Seiichi,Aono, Tetsuya
, p. 255 - 273 (2007/10/03)
A series of TAN-1511 analogues bearing a non-peptide spacer in place of the Gly-Gly-Gly sequence in the peptide moiety was synthesized, and the effects of these compounds on the proliferation of bone marrow cells in culture and experimental leukocytopenia in mice were examined. The structure- activity relationships obtained were as follows. As the substituent at the 2- position of the 4-thiabeptanoic acid framework, an amino group, methyl group or hydrogen was preferable; as a spacer in place of the Gly-Gly-Gly sequence, a 4-aminobenzoyl or 4-aminomethylbenzoyl group was suitable; and as the fatty acids bonded to the 6,7-dihydroxy groups, C16 fatty acid was best. Compounds 12f, 30d and 30i potently promoted the proliferation of bone marrow cells in culture and the restoration of leukocyte counts in a murine leukocytopenia model.
SYNTHESIS OF AN N-MUSTARD PRODRUG
Mann, John,Haase-Held, Margret,Springer, Caroline J.,Bagshawe, Kenneth D.
, p. 5377 - 5382 (2007/10/02)
We describe the synthesis of the novel N-mustard prodrug 4-benzoyl-L-glutamic acid, which is designed for activation by tumour localising antibody-carboxypeptidase conjugates.
Novel Prodrugs Which Are Activated to Cytotoxic Alkylating Agents by Carboxypeptidase G2
Springer, Caroline J.,Antoniw, Pari,Bagshawe, Kenneth D.,Searle, Frances,Bisset, Graham M. F.,Jarman, Michael
, p. 677 - 681 (2007/10/02)
The synthesis of three novel prodrugs, 4-amino>benzoyl-L-glutamic acid (7), 4-amino>benzoyl-L-glutamic acid (8), and 4-benzoyl-L-glutamic acid (9), for use as anticancer ag
Chemistry and Antitumor Evaluation of Selected Classical 2,4-Diaminoquinazoline Analogues of Folic Acid
Hynes, J.B.,Harmon, S.J.,Floyd, G.G.,Farrington, M.,Hart, L.D.,et al.
, p. 209 - 215 (2007/10/02)
A series of six 2,4-diaminoquinazoline analogues of folic acid which bear close structural resemblance to methotrexate, 1a, were synthesized by unequivocal routes.Three of these have not been described previously, while complete structural characterizatio
