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Within the limits of experimental error, the title compounds withD-confi guration displayed better antitumor activities against Bcap37 compared to their respective L -counterparts e.g. D-II a(52.3%) > L- II a (16.9%),D-II e (70.2%)> L-II e (25.9%), D-IIi (34.0%) >L-II i (26.1%). Furthermore, the compound bearing a fl uorine atom at the 4-position of the benzyl ring linked to the nitrogen atom of theamide (R1= p -F) showed good antitumor activities with inhibition rate ranging from 55.7 to 89.1% against BGC823 cell lines. With regard to the alkyl substituents (R2) in the phosphonate part of the studied compounds, D-diastereoisomers with diethyl substituents (R2 =Et) displayed signi fi cant enhancement towards inhibition against Bcap37, PC3 and BGC823 cells in comparison with D- O,O-dialkylphosphonates derived from n-propyl, isopropyl or n–butyl groups. In particular, the compound D-IIe(R1 =o -F, R2 = Et) dis-played most promising result amongst all. The L –diastereoisomers of O,O-diisopropylphosphonate e.g. L -II k(R1 = p-F, R2 = i-Pr), L -IIc(R1 = H, R2=i-Pr), L -II g(R1=o-F, R2=i-Pr), on the other hand,revealed higher antitumor activities than the L-diastereoisomers of phosphonates derived from ethyl,n -propyl or butyl groups (R2= Et, n-Pr, Bu). Thus, the nature of stereochemical con fi guration (D or L ) of the amino acid amide part, type of substituents (R1) in the aromatic ring as well as alkyl substituents (R2) in the phosphonate moiety of the title compounds appear to be the key factors in controlling the antitumor activity. While phosphonates derived from branched alkyl chains were preferred over straight-chain alkyls forL-diastereoisomers, simple diethyl derived phosphonates gave better result with D-diastereoisomers. Therefore, for ideal activity, R1should be a strong electron withdrawing group and for L-diastereoisomers R2 should be i-Pr, whereas for D -diastereoiso-mers R2 needs to be Et. Although our studies indicate the existence of a definite relationship of antitumor activity with the nature of substituents and type of confi guration within the compound, the role of steric, electronic and hydrophobic effects at physiological pH on structureeactivity relationships could not be successfully ascertained due to lack of structural diversity.   |
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此外, 酰胺(R1= p -F) 氮原子上苯环的4位上具有氟原子的化合物具有良好的抗肿瘤活性, 其对BGC823肿瘤细胞株的抑制率在55.7%到89.1%之间. 关于所研究化合物磷酸酯部分的烷基取代基(R2),二乙基取代(R2 =Et) 得到的D构型的非对映异构体相比由正丙基,异丙基和正丁基取代得到的二烷基磷酸酯, 能更显著地抑制Bcap37, PC3 和BGC823肿瘤细胞株. 尤其是化合物D-IIe(R1 =o -F, R2 = Et)最有潜力. 另一方面,L构型的二异丙基磷酸酯, 如L -II k(R1 = p-F, R2 = i-Pr), L -IIc(R1 = H, R2=i-Pr), L -II g(R1=o-F, R2=i-Pr), 比由乙基,正丙基或正丁基取代生成的磷酸酯具有更高的抗肿瘤活性. 因此,化合物氨基酸酰胺部分的立体化学构象(D 或 L), 芳香环上取代基的类型(R1)以及磷酸酯基团的烷基取代基种类(R2)都是控制其抗肿瘤活性的关键因素. 尽管对于L构型的非对映异构体,支链烷基衍生的磷酸酯比直链烷基的衍生物更具优势,但是在D构型时,简单的二乙基取代得到的结果更佳. 因此,要得到理想的抗肿瘤活性,R1必须是一个强吸电子基团,R2在L构型时应该是异丙基,而在D构型时应该是乙基. 尽管本研究表明化合物取代基的化学本质和构型与其抗肿瘤活性之间存在确定的关系, 然而由于所研究的结构多样性不足, 空间位阻, 电子和疏水作用在生理PH条件下在构效关系中所起的作用尚无法(成功)确定. I hope the above translaton helps. |
5楼2013-01-12 09:44:55
