Reference

4-Anilinoquinazolines with Lavendustin A subunit as inhibitors of epidermal growth factor receptor tyrosine kinase: syntheses, chemical and pharmacological properties

4-Anilinoquinazolines with Lavendustin A subunit as inhibitors of epidermal growth factor receptor tyrosine kinase: syntheses, chemical and pharmacological properties. Albuschat, Rica; Loewe, Werner; Weber, Manuela; Luger, Peter; Jendrossek, Verena (Institute of Pharmacy, Free University of Berlin, Berlin 14195, Germany). European Journal of Medicinal Chemistry, 39(12), 1001-1011 (English) 2004 Elsevier Ltd. CODEN: EJMCA5. ISSN: 0223-5234. DOCUMENT TYPE: Journal CA Section: 26 (Biomolecules and Their Synthetic Analogs) Section cross-reference(s): 1, 75 4-Anilinoquinazoline derivs. are widely investigated due to their potent epidermal growth factor receptor (EGFR) tyrosine kinase inhibitory activity. Two 4-anilinoquinazolines with Lavendustin A subunit I (R = Br, R1 = H; R = Cl, R1 = F) were synthesized and examd. for their EGFR tyrosine kinase inhibitory activity as well as their antiproliferative properties on variant human cancer cell lines. Both compds. maintained their EGFR tyrosine kinase inhibitory activity at the 10-7 M level and led to significant growth inhibition in certain leukemia, non-small cell lung cancer (NSCLC), ovarian cancer, renal cancer and breast cancer cell lines with GI50 values at the 10-6 M level. There could not be obsd. any notable difference between I regarding to their antiproliferative activity. The high tendency of I to include certain solvents, e.g.Several substances with their cas registry numbers 267243-28-7 and 828247-20-7 may be metioned in this study. water, DMF, DMSO, which may be due to the remarkable no. of hydrogen accepting/donating groups in 10a and b. An X-ray anal. of I (R = Br, R1 = H) including water and DMF illustrates a possible hydrogen bond pattern and could serve as information for preferred receptor (e.g. EGFR tyrosine kinase) binding sites. The p-quinone derivs., which contain a Michael acceptor position according to the irreversible EGFR tyrosine kinase inhibitor CI-1033, could be derived from the p-hydroquinone I, by oxidn. However, due to their instability the p-quinone derivs. could not be obtained in a pure form. .

Antitumor sustained-release injection containing vascular inhibitor

All Rights Reserved. Antitumor sustained-release injection containing vascular inhibitor. Kong, Qingzhong; He, Runping; Luan, Yongzu (Shandong Lan-Jin Bioengineering Co., Ltd., Peop. Rep. China). Faming Zhuanli Shenqing Gongkai Shuomingshu CN 1850048 A 25 Oct 2006, 36pp. (Chinese). (People's Republic of China). CODEN: CNXXEV. APPLICATION: CN 2010-200541 9 Jun 2006. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 The sustained-release injection is comprised of (A) sustained-release microsphere comprising antitumor effective constituent 0.5-60, sustained-release adjuvant 40-99% and suspending agent 0.0-30.0%; and (B) solvent. The antitumor effective constituent is selected from vascular inhibitor and/or taxane and alkylating agent and/or plant alkaloid. Said vascular inhibitor is selected from gefitinib, tarceva, lapatinib, angiostatin, avastin, canertinib, panitumumab, etc., or the mixt. thereof. Said taxane is selected from one of taxol, docetaxel, paclitaxel-2'-hydroxy, 10-deacetylbaccatin III, or 7-epi-taxol. Said alkylating agent is selected from one of ambamustine, nimustine, bendamustine, lomustine, tallimustine, melphalan, etc., or the mixt. thereof. Said plant alkaloid is selected from one of vincristine, vinblastine, vinleurosine, monocrotaline, etc., or the mixt. thereof. The sustained-release adjuvant is selected from one of (a) polylactic acid; (b) Polyglycolic acid-hydroxy acetic acid copolymer; (c) polifeprosan; (d) ethene-vinyl acetate copolymer; (e) difatty acid-sebacic acid copolymer; (f) poly(erucic acid dimer-sebacic acid) copolymer; (g) poly(fumaric acid-sebacic acid) copolymer; (h) sodium CM-cellulose, hydroxypropyl cellulose, xylitol, oligosaccharide, chondroitin, chitin, hyaluronic acid, collagens, etc.; or (i) racemic polylactic acid, etc., or the mixt. thereof. The suspending agent is one of (a) 0.5-3.0 % (sodium) CM-cellulose; (b) 5-15 % mannitol; (c) 5-15 % sorbitol; (d) 0.1-1.5 % surfactant; (e) 0.1-0.5 % tween 20; (f) (iodine) glycerin, dimethicone, propylene glycol, or carbomer; (g) 0.5-5 % sodium CM-cellulose + 0.1-0.5 % tween 80; (h) 5-20 % mannitol + 0. 267243-28-7 and 709611-53-0 which are cas registry numbers of substances are two of reagents here.1-0.5 % tween 80; or (i) 0.5-5 % sodium CM-cellulose + 5-20 % sorbitol + 0.1-0.5 % tween 80. The product can inhibit tumor cell and blood vessel, also can increase local concn. and enhance therapeutical effect. .