Synthesis antitumor drugs

Mitochondrial monoamine oxidase, 1, 253 Mitomycin synthesis, 7, 658, 659 Mitomycin-A, 7, 93 Mitomycin-B, 7, 93 Mitomycin-C, 7, 93 as antitumor drug, 4, 374 Mixed function oxidases, 1, 224 Mobam... 

Let s start with three examples of antitumor drugs that work by the inhibition of DNA synthesis methotrexate (MTX, Methopterin), 5-fluorouracil (Fluril), and 6-mercaptopurine (Purinethol). These are all old cancer drags, marketed under numerous trade names, including those indicated above. Although the mechanism of action of each one is different, at the end of the day they all inhibit DNA synthesis. 

Casiano Torres, C. A. and Baez, A. 1986. Effects of the antitumor drugs 3-nitrobenzothiallozo[3,2-a]quinolium and fagaronine on nucleic acid and protein synthesis. Biochemistry and Pharmacology, 35 679-685. 

An important application of the trans effect is the synthesis of specific isomers of coordination compounds. Equations (3) and (4) show how the cis and trans isomers of Pt(NH3)2Cl2 can be prepared selectively by taking advantage of the trans effect order Cl > NH3. This example is also of practical interest because the cis isomer is an important antitumor drug, but the trans isomer is ineffective. In each case the first step of the substitution can give only one isomer. In equation (3) the cis isomer is formed in the second step because the Cl trans to Cl is more labile than the Cl trans to the lower trans effect ligand, ammonia. On the other hand, in equation (4) the first Cl to substitute labilizes the ammonia trans to itself to give the trans dichloride as final product. 

The total synthesis of the microtubule stabilizing antitumor drug epothilone B was achieved by J. Mulzer et al. who cyclized the 16-membered macrocycle using the Keck macroiactonization. ... 

The objective of this review article is to provide comprehensive information about isolation, total synthesis, antitumor activity, and structure-activity relationship (SAR) correlations of tylophorinc-related alkaloids in order to facilitate the anticipated drug discovery and development of the tylophora class. 

The new antitumor drug Ag-7352 464 was designed based on 1,8-naphthyridin-2-one-3-carboxylic acid (1999MI4, 1999MI5). An efficient stereospecific procedure was specially developed for the synthesis of (iS, iS )-3-methoxy-4-methylaminopyrrolidine, the key reagent in the synthesis of naphthyridine 464 (2001TA1793). 

Synthesis of an analog of the antitumor drug methotrexate (154) is accomplished via condensation of the amino diester (152) and 4-amino-4-deoxy-Af-methylpteronic acid (153) in the presence of DEPC.60,61... 

MAJOR USES Used primarily in laboratories synthesis of diazomethane, cancer chemotherapy agent, mutagenic effects on plants and antitumoral drug. 

Huo M, Zhang Y et al (2010) Synthesis and characterization of low-toxic amphiphilic chitosan derivatives and their application as micelle carrier for antitumor drug. Int J Pharm 394 162-173... 

---