CN1278172A - 用于调制丝氨酸/苏氨酸蛋白激酶功能的氮杂苯并咪唑类化合物 - Google Patents
用于调制丝氨酸/苏氨酸蛋白激酶功能的氮杂苯并咪唑类化合物 Download PDFInfo
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- CN1278172A CN1278172A CN98810753A CN98810753A CN1278172A CN 1278172 A CN1278172 A CN 1278172A CN 98810753 A CN98810753 A CN 98810753A CN 98810753 A CN98810753 A CN 98810753A CN 1278172 A CN1278172 A CN 1278172A
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Abstract
Description
化合物编号 | R1 | X1 | R4 | Z3 |
A-1 | 苯基 | O | - | - |
A-2 | 苯基 | S | - | - |
A-3 | 苯基 | O | 甲基 | O |
A-4 | 苯基 | O | 乙基 | O |
A-5 | 2-硝基苯基 | O | - | - |
A-6 | 3-硝基苯基 | O | - | - |
A-7 | 4-硝基苯基 | O | - | - |
A-8 | 2-氯苯基 | O | - | - |
A-9 | 3-氯苯基 | O | - | - |
A-10 | 4-氯苯基 | O | - | - |
A-11 | 2-甲基苯基 | O | - | - |
A-12 | 3-甲基苯基 | O | - | - |
A-13 | 4-甲基苯基 | O | - | - |
A-14 | 2-氟苯基 | O | - | - |
A-15 | 3-氟苯基 | O | - | - |
A-16 | 4-氟苯基 | O | - | - |
A-17 | 2-(三氟甲基)苯基 | O | - | - |
A-18 | 3-(三氟甲基)苯基 | O | - | - |
A-19 | 4-(三氟甲基)苯基 | O | - | - |
A-20 | 2-甲氧基苯基 | O | - | - |
化合物编号 | R1 | X1 | R4 | Z3 |
A-21 | 3-甲氧基苯基 | O | - | - |
A-22 | 4-甲氧基苯基 | O | - | - |
A-23 | 2-羧基苯基 | O | - | - |
A-24 | 3-羧基苯基 | O | - | - |
A-25 | 4-羧基苯基 | O | - | - |
A-26 | 2-硝基苯基 | S | - | - |
A-27 | 3-硝基苯基 | S | - | - |
A-28 | 4-硝基苯基 | S | - | - |
A-29 | 2-氯苯基 | S | - | - |
A-30 | 3-氯苯基 | S | - | - |
A-31 | 4-氯苯基 | S | - | - |
A-32 | 2-甲基苯基 | S | - | - |
A-33 | 3-甲基苯基 | S | - | - |
A-34 | 4-甲基苯基 | S | - | - |
A-35 | 2-氟苯基 | S | - | - |
A-36 | 3-氟苯基 | S | - | - |
A-37 | 4-氟苯基 | S | - | - |
A-38 | 2-(三氟甲基)苯基 | S | - | - |
A-39 | 3-(三氟甲基)苯基 | S | - | - |
A-40 | 4-(三氟甲基)苯基 | S | - | - |
A-41 | 2-甲氧基苯基 | S | - | - |
A-42 | 3-甲氧基苯基 | S | - | - |
A-43 | 4-甲氧基苯基 | S | - | - |
A-44 | 2-羧基苯基 | S | - | - |
A-45 | 3-羧基苯基 | S | - | - |
A-46 | 4-羧基苯基 | S | - | - |
化合物编号 | R1 | X1 | R4 | Z3 |
A-47 | 苯基 | NH | - | - |
A-48 | 2-硝基苯基 | NH | - | - |
A-49 | 3-硝基苯基 | NH | - | - |
A-50 | 4-硝基苯基 | NH | - | - |
A-51 | 2-氯苯基 | NH | - | - |
A-52 | 3-氯苯基 | NH | - | - |
A-53 | 4-氯苯基 | NH | - | - |
A-54 | 2-甲基苯基 | NH | - | - |
A-55 | 3-甲基苯基 | NH | - | - |
A-56 | 4-甲基苯基 | NH | - | - |
A-57 | 2-氟苯基 | NH | - | - |
A-58 | 3-氟苯基 | NH | - | - |
A-59 | 4-氟苯基 | NH | - | - |
A-60 | 2-(三氟甲基)苯基 | NH | - | - |
A-61 | 3-(三氟甲基)苯基 | NH | - | - |
A-62 | 4-(三氟甲基)苯基 | NH | - | - |
A-63 | 2-甲氧基苯基 | NH | - | - |
A-64 | 3-甲氧基苯基 | NH | - | - |
A-65 | 4-甲氧基苯基 | NH | - | - |
A-66 | 2-羧基苯基 | NH | - | - |
A-67 | 3-羧基苯基 | NH | - | - |
A-68 | 4-羧基苯基 | NH | - | - |
A-69 | 2-硝基苯基 | O | 甲基 | O |
A-70 | 3-硝基苯基 | O | 甲基 | O |
A-71 | 4-硝基苯基 | O | 甲基 | O |
A-72 | 2-氯苯基 | O | 甲基 | O |
化合物编号 | R1 | X1 | R4 | Z3 |
A-73 | 3-氯苯基 | O | 甲基 | O |
A-74 | 4-氯苯基 | O | 甲基 | O |
A-75 | 2-甲基苯基 | O | 甲基 | O |
A-76 | 3-甲基苯基 | O | 甲基 | O |
A-77 | 4-甲基苯基 | O | 甲基 | O |
A-78 | 2-氟苯基 | O | 甲基 | O |
A-79 | 3-氟苯基 | O | 甲基 | O |
A-80 | 4-氟苯基 | O | 甲基 | O |
A-81 | 2-(三氟甲基)苯基 | O | 甲基 | O |
A-82 | 3-(三氟甲基)苯基 | O | 甲基 | O |
A-83 | 4-(三氟甲基)苯基 | O | 甲基 | O |
A-84 | 2-甲氧基苯基 | O | 甲基 | O |
A-85 | 3-甲氧基苯基 | O | 甲基 | O |
A-86 | 4-甲氧基苯基 | O | 甲基 | O |
A-87 | 2-羧基苯基 | O | 甲基 | O |
A-88 | 3-羧基苯基 | O | 甲基 | O |
A-89 | 4-羧基苯基 | O | 甲基 | O |
A-90 | 苯基 | S | 甲基 | O |
A-91 | 2-硝基苯基 | S | 甲基 | O |
A-92 | 3-硝基苯基 | S | 甲基 | O |
A-93 | 4-硝基苯基 | S | 甲基 | O |
A-94 | 2-氯苯基 | S | 甲基 | O |
A-95 | 3-氯苯基 | S | 甲基 | O |
A-96 | 4-氯苯基 | S | 甲基 | O |
A-97 | 2-甲基苯基 | S | 甲基 | O |
A-98 | 3-甲基苯基 | S | 甲基 | O |
化合物编号 | R1 | X1 | R4 | Z3 |
A-99 | 4-甲基苯基 | S | 甲基 | O |
A-100 | 2-氟苯基 | S | 甲基 | O |
A-101 | 3-氟苯基 | S | 甲基 | O |
A-102 | 4-氟苯基 | S | 甲基 | O |
A-103 | 2-(三氟甲基)苯基 | S | 甲基 | O |
A-104 | 3-(三氟甲基)苯基 | S | 甲基 | O |
A-105 | 4-(三氟甲基)苯基 | S | 甲基 | O |
A-106 | 2-甲氧基苯基 | S | 甲基 | O |
A-107 | 3-甲氧基苯基 | S | 甲基 | O |
A-108 | 4-甲氧基苯基 | S | 甲基 | O |
A-109 | 2-羧基苯基 | S | 甲基 | O |
A-110 | 3-羧基苯基 | S | 甲基 | O |
A-111 | 4-羧基苯基 | S | 甲基 | O |
A-112 | 苯基 | NH | 甲基 | O |
A-113 | 2-硝基苯基 | NH | 甲基 | O |
A-114 | 3-硝基苯基 | NH | 甲基 | O |
A-115 | 4-硝基苯基 | NH | 甲基 | O |
A-116 | 2-氯苯基 | NH | 甲基 | O |
A-117 | 3-氯苯基 | NH | 甲基 | O |
A-118 | 4-氯苯基 | NH | 甲基 | O |
A-119 | 2-甲基苯基 | NH | 甲基 | O |
A-120 | 3-甲基苯基 | NH | 甲基 | O |
A-121 | 4-甲基苯基 | NH | 甲基 | O |
A-122 | 2-氟苯基 | NH | 甲基 | O |
A-123 | 3-氟苯基 | NH | 甲基 | O |
A-124 | 4-氟苯基 | NH | 甲基 | O |
化合物编号 | R1 | X1 | R4 | Z3 |
A-125 | 2-(三氟甲基)苯基 | NH | 甲基 | O |
A-126 | 3-(三氟甲基)苯基 | NH | 甲基 | O |
A-127 | 4-(三氟甲基)苯基 | NH | 甲基 | O |
A-128 | 2-甲氧基苯基 | NH | 甲基 | O |
A-129 | 3-甲氧基苯基 | NH | 甲基 | O |
A-130 | 4-甲氧基苯基 | NH | 甲基 | O |
A-131 | 2-羧基苯基 | NH | 甲基 | O |
A-132 | 3-羧基苯基 | NH | 甲基 | O |
A-133 | 4-羧基苯基 | NH | 甲基 | O |
A-134 | 2-硝基苯基 | O | 乙基 | O |
A-135 | 3-硝基苯基 | O | 乙基 | O |
A-136 | 4-硝基苯基 | O | 乙基 | O |
A-137 | 2-氯苯基 | O | 乙基 | O |
A-138 | 3-氯苯基 | O | 乙基 | O |
A-139 | 4-氯苯基 | O | 乙基 | O |
A-140 | 2-甲基苯基 | O | 乙基 | O |
A-141 | 3-甲基苯基 | O | 乙基 | O |
A-142 | 4-甲基苯基 | O | 乙基 | O |
A-143 | 2-氟苯基 | O | 乙基 | O |
A-144 | 3-氟苯基 | O | 乙基 | O |
A-145 | 4-氟苯基 | O | 乙基 | O |
A-146 | 2-(三氟甲基)苯基 | O | 乙基 | O |
A-147 | 3-(三氟甲基)苯基 | O | 乙基 | O |
A-148 | 4-(三氟甲基)苯基 | O | 乙基 | O |
A-149 | 2-甲氧基苯基 | O | 乙基 | O |
A-150 | 3-甲氧基苯基 | O | 乙基 | O |
化合物编号 | R1 | X1 | R4 | Z3 |
A-151 | 4-甲氧基苯基 | O | 乙基 | O |
A-152 | 2-羧基苯基 | O | 乙基 | O |
A-153 | 3-羧基苯基 | O | 乙基 | O |
A-154 | 4-羧基苯基 | O | 乙基 | O |
A-155 | 苯基 | S | 乙基 | O |
A-156 | 2-硝基苯基 | S | 乙基 | O |
A-157 | 3-硝基苯基 | S | 乙基 | O |
A-158 | 4-硝基苯基 | S | 乙基 | O |
A-159 | 2-氯苯基 | S | 乙基 | O |
A-160 | 3-氯苯基 | S | 乙基 | O |
A-161 | 4-氯苯基 | S | 乙基 | O |
A-162 | 2-甲基苯基 | S | 乙基 | O |
A-163 | 3-甲基苯基 | S | 乙基 | O |
A-164 | 4-甲基苯基 | S | 乙基 | O |
A-165 | 2-氟苯基 | S | 乙基 | O |
A-166 | 3-氟苯基 | S | 乙基 | O |
A-167 | 4-氟苯基 | S | 乙基 | O |
A-168 | 2-(三氟甲基)苯基 | S | 乙基 | O |
A-169 | 3-(三氟甲基)苯基 | S | 乙基 | O |
A-170 | 4-(三氟甲基)苯基 | S | 乙基 | O |
A-171 | 2-甲氧基苯基 | S | 乙基 | O |
A-172 | 3-甲氧基苯基 | S | 乙基 | O |
A-173 | 4-甲氧基苯基 | S | 乙基 | O |
A-174 | 2-羧基苯基 | S | 乙基 | O |
A-175 | 3-羧基苯基 | S | 乙基 | O |
A-176 | 4-羧基苯基 | S | 乙基 | O |
化合物编号 | R1 | X1 | R4 | Z3 |
A-177 | 苯基 | NH | 乙基 | 0 |
A-178 | 2-硝基苯基 | NH | 乙基 | 0 |
A-179 | 3-硝基苯基 | NH | 乙基 | 0 |
A-180 | 4-硝基苯基 | NH | 乙基 | O |
A-181 | 2-氯苯基 | NH | 乙基 | 0 |
A-182 | 3-氯苯基 | NH | 乙基 | O |
A-183 | 4-氯苯基 | NH | 乙基 | 0 |
A-184 | 2-甲基苯基 | NH | 乙基 | O |
A-185 | 3-甲基苯基 | NH | 乙基 | 0 |
A-186 | 4-甲基苯基 | NH | 乙基 | 0 |
A-187 | 2-氟苯基 | NH | 乙基 | 0 |
A-188 | 3-氟苯基 | NH | 乙基 | 0 |
A-189 | 4-氟苯基 | NH | 乙基 | O |
A-190 | 2-(三氟甲基)苯基 | NH | 乙基 | O |
A-191 | 3-(三氟甲基)苯基 | NH | 乙基 | 0 |
A-192 | 4-(三氟甲基)苯基 | NH | 乙基 | 0 |
A-193 | 2-甲氧基苯基 | NH | 乙基 | 0 |
A-194 | 3-甲氧基苯基 | NH | 乙基 | 0 |
A-195 | 4-甲氧基苯基 | NH | 乙基 | 0 |
A-196 | 2-羧基苯基 | NH | 乙基 | O |
A-197 | 3-羧基苯基 | NH | 乙基 | 0 |
A-198 | 4-羧基苯基 | NH | 乙基 | O |
化合物 | IC50(μM) |
A-1 | 79 |
A-2 | >100 |
A-3 | 6.1 |
A-4 | 6.7 |
A-90 | 0.95 |
化合物 | IC50(μM) |
A-1 | >100 |
A-2 | >100 |
A-3 | >100 |
A-4 | >100 |
化合物 | IC50(μM)RAS/NIH3T3 |
A-3 | 40 |
A-4 | 20 |
化合物 | IC50(μM)A549 |
A-3 | 2265(2%FBS) |
A-4 | 65.7(2%FBS) |
Claims (37)
Applications Claiming Priority (2)
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US6014597P | 1997-09-26 | 1997-09-26 | |
US60/060,145 | 1997-09-26 |
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