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首页> 外文期刊>Journal of chemical crystallography >Tyrphostin tumor growth inhibitors of EGFR and ErbB2 tyrosine kinase
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Tyrphostin tumor growth inhibitors of EGFR and ErbB2 tyrosine kinase

机译：Tyrphostin EGFR和ErbB2酪氨酸激酶的肿瘤生长抑制剂

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Tyrosine kinase inhibitors are small molecules that bind to the ATP binding site of the tyrosine kinase domain of the epidermal growth factor receptor (EGFR) and disrupt the uncontrolled signaling reactions in cancer cells by inhibiting tyrosine phosphorylation. Tyrphostins (or malononitriles) are one class of compounds known to function as tyrosine kinase inhibitors. Our focus is to determine the structural features of these molecules that make them candidates for tyrosine kinase inhibitors. In this study, the X-ray crystal structures of four compounds shown to have EGFR tyrosine kinase inhibition have been determined. They are 4-methoxybenzylidenemalononitrile, (3,4,5-trihydroxybenzylidene)malononitrile, alpha-cyano-(3,5-di-t-butyl-4-hydroxy)thiocinnamide, and N-(3',4'-dihydroxybenzylidenecyanoacetyl)indoline. Crystallographic data: 4-methoxybenzylidenemalononitrile, P2(1)/c, a = 3.9173(6) angstrom, b = 24.909(3) angstrom, c = 9.6487(9) angstrom, beta = 91.10(1)degrees, V = 941.3(2) angstrom(3); (3,4,5-trihydroxybenzylidene) malononitrile, P2(1)/c, a = 7.0065(5) angstrom, b = 10.7158(9) angstrom, c = 13.4191(10) angstrom, beta = 102.986(6)degrees, V = 981.7(1) angstrom(3); alpha-cyano-(3,5-di-t-butyl-4- hydroxy)thiocinnamide, P1bar, a = 9.6640(19) angstrom, b = 9.7204(13) angstrom, c = 10.3305(18) angstrom, alpha= 88.93(1)degrees, beta= 83.88(2)degrees, gamma= 66.12(1)degrees, V = 882.0(3) angstrom(3); N-(3',4'-dihydroxybenzylidenecyanoacetyl)indoline, P1bar, a = 7.8887(7) angstrom, b = 8.220(1) angstrom, c = 12.967(2) angstrom, alpha= 94.42(1)degrees, beta= 99.45(9)degrees, gamma= 118.37(8)degrees, V = 718.0(2) angstrom(3).
机译：酪氨酸激酶抑制剂是与表皮生长因子受体（EGFR）的酪氨酸激酶结构域的ATP结合位点结合的小分子，并通过抑制酪氨酸磷酸化来破坏癌细胞中不受控制的信号传导反应。酪氨酸磷酸化抑制剂（或丙二腈）是一类已知起酪氨酸激酶抑制剂作用的化合物。我们的重点是确定这些分子的结构特征，使其成为酪氨酸激酶抑制剂的候选者。在这项研究中，已确定了四种具有EGFR酪氨酸激酶抑制作用的化合物的X射线晶体结构。它们是4-甲氧基苄基亚甲基丙二腈，（3,4,5-三羟基亚苄基）丙二腈，α-氰基-（3,5-二叔丁基-4-羟基）硫辛酰胺和N-（3'，4'-二羟基苄基亚氰基乙酰基）吲哚啉。晶体学数据：4-甲氧基亚苄基丙二腈，P2（1）/ c，a = 3.9173（6）埃，b = 24.909（3）埃，c = 9.6487（9）埃，β= 91.10（1）度，V = 941.3（ 2）埃（3）; （3,4,5-三羟基亚苄基）丙二腈，P2（1）/ c，a = 7.0065（5）埃，b = 10.7158（9）埃，c = 13.4191（10）埃，beta = 102.986（6）度， V = 981.7（1）埃（3）; α-氰基-（3,5-二叔丁基-4-羟基）硫辛酰胺，P1bar，a = 9.6640（19）埃，b = 9.7204（13）埃，c = 10.3305（18）埃，α= 88.93 （1）度，beta = 83.88（2）度，γ= 66.12（1）度，V = 882.0（3）埃（3）; N-（3'，4'-二羟基亚苄基氰基乙酰基）二氢吲哚，P1bar，a = 7.8887（7）埃，b = 8.220（1）埃，c = 12.967（2）埃，alpha = 94.42（1）度，beta = 99.45 （9）度，gamma = 118.37（8）度，V = 718.0（2）埃（3）。

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