ライフサイエンスコーパス: combretastatin

1 rization with activity comparable to that of combretastatin A-1 (3a), the phosphorylated derivative (

2 activity, and the benzophenone derivative of combretastatin A-1 was therefore synthesized.

3 t, the corresponding carbonate derivative of combretastatin A-4 (13) was unstable in aqueous environm

4 eries of cis- and trans-stilbenes related to combretastatin A-4 (1a), with a variety of substituents

5 ombretum caffrum) antineoplastic constituent combretastatin A-4 (1b) directed at maintaining the (Z)-

6 y crystal structure of the 3'-O-phosphate of combretastatin A-4 (1b) was successfully elucidated.

7 nding of colchicine to tubulin comparable to combretastatin A-4 (1b).

8 sent SAR studies of the antineoplastic agent combretastatin A-4 (1c) were focused mainly on the olefi

9 served with the phosphorylated derivative of combretastatin A-4 (1d), phosphate 3d retained detectabl

10 ombretum caffrum) antineoplastic constituent combretastatin A-4 (3b) led to the discovery of a potent

11 phenolic anticancer drugs etoposide (6) and combretastatin A-4 (7) were attached to the Z-val-cit-p-

12 y-1H-indoles were obtained as a new class of combretastatin A-4 (CA-4) analogues via a convenient ult

13 eric derivatives designed as cis-constrained combretastatin A-4 (CA-4) analogues were synthesized and

14 Cis-stilbene combretastatin A-4 (CA-4) and a large group of its deriv

15 Evidence accumulated with combretastatin A-4 (CA-4) and its prodrug CA-4P support

16 erocycles in place of the cis double bond in combretastatin A-4 (CA-4) are described.

17 Combretastatin A-4 (CA-4) in phosphate and serine pro-dr

18 Combretastatin A-4 (CA-4) is a naturally occurring agent

19 iguration afforded by the cis double bond in combretastatin A-4 (CA-4).

20 embly with IC50 values comparable to that of combretastatin A-4 (CA-4).

21 vel 2,5-diaryl-1,3,4-oxadiazoline analogs of combretastatin A-4 (CA-4, 1) were designed, synthesized,

22 A prodrug of combretastatin A-4 (CA4) was prepared, CMP-L-CA4, where

23 inoacrylate linker (L), and a cytotoxic drug combretastatin A-4 (CA4).

24 zole scaffold and designed as cis-restricted combretastatin A-4 analogues, was synthesized with the g

25 nt inhibition of tubulin polymerization than combretastatin A-4 and strong binding to the colchicine

26 mitotic natural products podophyllotoxin and combretastatin A-4 and to that of NSC 664171, a particul

27 embranes, which was similar to cisplatin and combretastatin A-4 and without significant toxicity towa

28 Compounds 9i and j were more active than combretastatin A-4 as inhibitors of tubulin polymerizati

29 rowth and, potentially, to better define the combretastatin A-4 binding site on tubulin.

30 The mechanism of combretastatin A-4 cytotoxicity has now been investigate

31 Incubation of cells for up to 8 h with combretastatin A-4 did not induce the release of lactate

32 The antiangiogenic, tubulin-binding drug combretastatin A-4 exhibits a selective toxicity for pro

33 was detected in cells incubated with 0.1 mM combretastatin A-4 for 24 h.

34 totoxic and antitubulin activity compared to combretastatin A-4 in neuroblastoma cells, showing a bet

35 n was confirmed, and it was more potent than combretastatin A-4 in these assays.

36 Incubation of cells with 0.1 mM combretastatin A-4 induced the conversion (first detecte

37 icate that the selective cytotoxic effect of combretastatin A-4 is mediated by the induction of apopt

38 tected with either the colchicine site agent combretastatin A-4 or with an analog of the antimitotic

39 and the cancer antiangiogenesis drug sodium combretastatin A-4 phosphate (2b), syntheses of certain

40 Combretastatin A-4 phosphate (CA4P) is a novel antitumor

41 Purpose To determine if combretastatin A-4 phosphate disodium (CA4P) can enhance

42 nd is achievable with at least three agents, combretastatin A-4 phosphate, pigment epithelium-derived

43 del comparable to the activity obtained with combretastatin A-4 phosphate.

44 Compound 1b has been termed the "combretastatin A-4 prodrug", and it is currently undergo

45 This benzophenone derivative of combretastatin A-4 showed remarkable antineoplastic acti

46 expectedly obtained by Jacobsen oxidation of combretastatin A-4 silyl ether (1c --> 3a), and the pare

47 The geometric trans-isomer 3a of combretastatin A-4 was converted to the (1S,2S)- and (1R

48 ion (IC50 = 22 microM, versus 1.2 microM for combretastatin A-4), while 4d was inactive (IC50 > 40 mi

49 structure of a known microtubule inhibitor, combretastatin A-4, Borowiak et al. develop a photoswitc

50 ture of the tubulin polymerization inhibitor combretastatin A-4, the possibility exists that the rati

51 Combretastatin A-4-phosphate (CA-4-P) is a tubulin-bindi

52 The tubulin-binding agent combretastatin A-4-phosphate (CA-4-P), rapidly disrupts

53 In this study the effect of a CA-4 prodrug, combretastatin A-4-phosphate (CA-4-P), was tested in two

54 cancer cells and superior to colchicine and combretastatin A-4.

55 tereoselective synthesis of anticancer agent combretastatin A-4.

56 arison with the potent colchicine site agent combretastatin A-4.

57 aqueous environments and was as cytotoxic as combretastatin A-4.

58 al products colchicine, podophyllotoxin, and combretastatin A-4.

59 to those of colchicine, podophyllotoxin, and combretastatin A-4.

60 al products colchicine, podophyllotoxin, and combretastatin A-4.

61 al products colchicine, podophyllotoxin, and combretastatin A-4.

62 series of carbazole sulfonamides related to Combretastatin A4 (1) were synthesized and evaluated for

63 of either anecortave acetate (300 microg) or combretastatin A4 (1.5 mg).

64 st potent compounds exceeded the activity of combretastatin A4 (CA-4), showing single digit nM IC50 v

65 Combretastatin A4 (CA4) phosphate (CA4P) inhibits microt

66 CA4P was rapidly converted to the active combretastatin A4 (CA4), which was further metabolized t

67 phorylation of the parent compound (CA4P) to combretastatin A4 (CA4), with a short plasma half-life (

68 small molecule VTAs: the antitubulin drugs, combretastatin A4 phosphate (CA4P) and ZD6126, and the f

69 ol was performed 24 hours after injection of combretastatin A4 phosphate (CA4P) in 12 mice.

70 ute effects of the vascular disrupting agent combretastatin A4 phosphate (CA4P) on luciferase-express

71 the effects of the vascular targeting agent combretastatin A4 phosphate (CA4P) on tumor and normal t

72 Vascular-disrupting agents (VDAs) such as combretastatin A4 phosphate (CA4P) selectively disrupt b

73 A phase I trial was performed with combretastatin A4 phosphate (CA4P), a novel tubulin-bind

74 cy of microtubule-disrupting agents, such as combretastatin A4 phosphate (CA4P), in inducing rapid re

75 The disodium combretastatin A4 phosphate prodrug is currently undergo

76 ons of the selective vascular-targeting drug combretastatin A4 prodrug (CA4P) or anecortave acetate,

77 In contrast, the vascular disrupting agent combretastatin A4-phosphate, which caused a similar amou

78 e development of one such antivascular drug, combretastatin A4.

79 eries of novel pyridine-bridged analogues of combretastatin-A4 (CA-4) were designed and synthesized.

80 tion on vascular and therapeutic response to combretastatin-A4 3-O-phosphate (CA-4-P), which was chos

81 xic doses of microtubule-destabilizing agent combretastatin-A4-phosphate (CA4P) inhibit leukemic cell

82 treatment with the vascular targeting agent, combretastatin A4P, or the antiangiogenic agent, contort

83 have developed a modular synthetic route to combretastatin analogs based on a pyrazole core through

84 iogenesis was inhibited after treatment with combretastatin and thalidomide.

85 w assesses the in vitro and in vivo data for combretastatin and the prodrug, and the preliminary data

86 The combretastatins are an important class of tubulin-bindin

87 of a new family of macrocyclic analogues of combretastatins B combining oxygenated substituents on t

88 The vasodisruptive drug combretastatin CA4 also targeted MV selectively but acte

89 D-2 and D-4 as well as a formal synthesis of combretastatin D-1 by a conceptually new route harnessin

90 ld be prepared as a side product en route to combretastatin D-2 by synchronous extrusion of SO2 and C

91 We report the syntheses of combretastatins D-2 and D-4 as well as a formal synthesi

92 Combretastatin has shown activity in phase 1 and phase I

93 arried out to develop a predictive model for combretastatin-like analogues populating the colchicine-

94 COMPARE analysis led to the discovery of a combretastatin-like quinoline-5,8-dione structure that,

95 have synthesized a novel class of cis-locked combretastatins named combreatabenzodiazepines.