Department of Pharmaceutical Chemistry, Institute of Health Biosciences, Graduate School of The University of Tokushima, 1-78, Sho-machi, Tokushima 770-8505, Japan.
Bioorg Med Chem. 2012 Sep 15;20(18):5559-67. doi: 10.1016/j.bmc.2012.07.031. Epub 2012 Jul 25.
Four kinds of symmetrically branched oligoglyceryl trimeric (BGL003)-paclitaxel conjugates and a corresponding heptameric (BGL007) conjugate were synthesized. Molecular weights of all the compounds were less than two times that of paclitaxel. The anti-tumor activity of the most water-soluble BGL003 conjugate was examined and found to be preserved in spite of the chemical modification that is displacement of the N3'-debenzoyl residue with the BGL003 succinyl residue.
四种对称支化的低聚甘油三聚体(BGL003)-紫杉醇缀合物和一种相应的七聚体(BGL007)缀合物被合成。所有化合物的分子量均小于紫杉醇的两倍。尽管进行了化学修饰,即用 BGL003 琥珀酰基取代了 N3'-去苯甲酰基,但最具水溶性的 BGL003 缀合物的抗肿瘤活性仍得以保留,并对其进行了检测。