Structure-activity relationships analogue

King, P., Ma, G., Miao, W., Jia, Q., McDougall, B., Reinecke, M., Cornell, C., Kuan, J., Kim, T., and Robinson, W. 1999. Structure-activity relationships analogues of the dicaffeoylquinic and dicaffeoyltartaric acids as potent inhibitors of human immunodeficiency virus type 1 integrase and replication. J. Med. Chem. 42, 497-509. 

Structure—Activity Relationships. In spite of the considerable synthetic and bioassay effort involved in estabhshing the thyromimetic potency of thyroid-hormone analogues, more than 100 compounds have been studied (Table 2). The main stmctural requirements for thyromimetic activity can be summarized as follows (6,12—16). 

The structure activity relationships ( SAR) of newly synthesized analogues of nucleosides, xanthine heterocycles, and nonxanthine heterocycles have been explored at the ARs. Potent and selective AR antagonists have been prepared for all four subtypes [3, 4], and selective agonists are known for three subtypes [1]. Thus, numerous pharmacological tools are available for in vitro and in vivo use (Table 2). Potent and selective A2b AR agonists are yet to be repotted, although several research groups have identified lead compounds. 

Medvedev AE, Veselovsky AV, Shvedov VI, Tikhonova OV, Moskvitina TA, Fedotova OA, et al. Inhibition of monoamine oxidase by pirlindole analogues 3D-QSAR and CoMFA analysis. / Chem Inf Comput Sci 1998 38 1137-44. Miller JR, Edmondson DE. Structure-activity relationships in the oxidation of para-substituted benzylamine analogues by recombinant human liver monoamine oxidase A. Biochemistry 1999 38 13670-83. 

In 1985, it was reported by Hsiang et al. [43] that the cytotoxic activity of 20-(S)-camptothecin (CPT III) was attributed to a novel mechanism of action involving the nuclear enzyme topo I, and this discovery of unique mechanism of action revived the interest in CPT and its analogues as anticancer agents. CPT stabilizes the covalent, reversible topo I-DNA complex leading to the inhibition of DNA synthesis in mammalian cells and interferes with the topo I breakage-reunion reaction [44]. Clinical trials and structure-activity relationships have demonstrated the requirement of the a-hydroxy group, the... 

Hellberg, S., Eriksson, L., Jonsson, J., Lindgren, F., Sjostrom, M., Skagerberg, B., Wold, S. and Andrews, P. (1991), Minimum analogue peptide sets (MAPS) for quantitative structure-activity relationships , Int.J. Peptide Protein Res., 37, 414-424. 

The range of these aza-ellipticine analogues, although by now extensive, is still insufficient to permit a systematic evaluation of their structure-activity relationships. It is established, however, that the three methylated compounds 11-13 are all less active than ellipticine toward a range of tumor cell lines <2004AP434>. 

Meyers MJ, Sun J, Carlson KE, Marriner A, Katznellenbogen BS, Katzenellenbogen JA (2001) Estrogen receptor-/ potency-selective ligands structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues. J Med Chem 44 4230-4251... 

Synthesis, cytotoxicity in vitro and in vivo, and structure-activity relationships of septicine 280 and its analogues were reported (Figure 7) <2003BML1679>. 

The most potent among the compounds tested were the pyridazi-nones (28, R1 = Ph, R2, R3, R4, R5 = H, n = 2-5) [101]. Structure-activity relationships have been investigated in detail with this type of compound. Also, thio-analogues of compounds (28) (3-pyridazinethione derivatives) as well as 2-aminoalky]-6-aryl-3(2//)-pyridazinones were claimed in patents as gastric secretion inhibitors or anti-ulcer agents [100, 102, 103]. 

Dequalinium salts can be purchased from Sigma Chemical Co., St. Louis, Missouri, U.S.A. Analogues of dequalinium, however, are not commercially available they can be synthesized according to protocols by Galanakis et al. (44 6). In a structure-activity relationship study (38), we found that the methyl group in ortho position to the quaternary nitrogen at the quinolinium ring system seems to play an essential role in the... 

Galanakis D, Davis CA, Del Rey Herrero B, Ganellin CR, Dunn PM, Jenkinson DH. Synthesis and structure-activity relationships of dequalinium analogues as K(+) channel blockers. Investigations on the role of the charged heterocycle. J Med Chem 1995 38 595-606. 

Cenci di Bello I, Fleet G Namgoong SK, Tadano K-I, Winchester B. (1989) Structure-activity relationship of swainsonine. Inhibition of human alpha-mannosidases by swainsonine analogues. BiochemJ 259 855-861. 

Guenard D, Gueritte-Voegelein F, Dubois J, Potter P. (1993) Structure-activity relationships of taxol and taxotere analogues. J Natl Cancer Inst Monogr 15 79-82. 

Yu QS, HoUoway HH, Flippen Anderson JL, et ai. Methyl analogues of the experimental Alzheimer drug phenserine. Synthesis and structure/activity relationships for acetyl- and butyrylchoHnesterase inhibitory action, / Chem 44 4062 071,2001. 

G. B. Evans, R. H. Fumeaux, A. Lewandowicz, V. L. Schramm, and P. C. Tyler, Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase, J. Med. Chem., 46 (2003) 3412-3423. 

Posner and coworkers have developed versatile methodology for the synthesis of novel 1,2,4-trioxanes that has allowed detailed investigation of their Structure-Activity Relationships (SAR) , while Jefford and coworkers first synthesized fenozan BO-7, so naturally some of their work has centered on its mechanism of action. Avery and coworkers have also contributed significantly to the area by the syntheses and QSAR (Quantitative SAR) studies of many artemisinin analogues. 

B. Resul, J. Stjernschantz, Structure-activity relationships of prostaglandin analogues as ocular hypotensive agents, Curr. Opin. Then Pat. 3 (1993) 781. 

R. Miller, D.E. Edmondson, Structure-activity relationships in the oxidation of para-substituted benzylamine analogues by recombinant human liver monoamine oxidase A, Biochemistry 38 (1999) 13670-13683. 

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