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In Vivo Methods for Screening and Preclinical Testing
The classic question in the field of drug discovery is: Which tumor model is a satis-factory predictor for cancer in humans? The classic answer is: None of them!
Transplantable Syngeneic Rodent Tumors
TLDR
This chapter is an effort to summarize some of the basic operating characteristics of a wide range of solid-tumor models and can best explainSome of the behavioral characteristics of these models within therapeutic experiments. Expand
6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors.
TLDR
Two analogues of AGF94 with a thienoyl side chain and three-carbon bridge lengths inhibited proliferation of Chinese hamster ovary sublines expressing folate receptors and inhibited glycinamide ribonucleotide formyltransferase (GARFTase). Expand
Discovery and Preclinical Antitumor Efficacy Evaluations of LY32262 and LY33169
TLDR
There was no absolute tissue of origin correlation with antitumor efficacy, although colon tumors were most responsive and mammary tumors least responsive, and the cause of the “hit and miss” efficacy has not been determined. Expand
Synthetic modification of the 2-oxypropionic acid moiety in 2-{4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy}propionic acid (XK469), and consequent antitumor effects. Part 4.
TLDR
The present work demonstrates that substitution of fluorine at the 3-position of the 1,4-OC(6)H(4)O-linker of XK469 leads to a 10-fold reduction in activity, whereas the corresponding 2-fluoro analog proved to be 100-fold less active than Xk469. Expand
Preclinical antitumor efficacy of analogs of XK469: sodium-(2-[4-(7-chloro-2-quinoxalinyloxy)phenoxy]propionate
TLDR
Assure® had no selective cytotoxicity for solid tumors in the disk-assay, and was devoid of antitumor activity, while the analog XK469 is in clinical development. Expand
Transplantable Syngeneic Rodent Tumors: Solid Tumors in Mice
TLDR
This work presents what it hopes will be useful information regarding the transplant characteristics of tumor models, with some of the “pitfalls” to look out for when using any given tumor model for chemotherapy evaluations. Expand
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
TLDR
An effort was initiated to establish a pharmacophore hypothesis to delineate the requirements of the active site, via a comprehensive program of synthesis of analogues of XK469 and evaluation of the effects of structural modification(s) on solid tumor activity. Expand
Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors
TLDR
In SCID mice with KB tumors, 1 was highly active against both early and advanced stage tumors, and in vivo antitumor activity for 1 due to selective transport by FRs and PCFT over RFC was demonstrated. Expand
Cryptophycins-309, 249 and other cryptophycin analogs: Preclinical efficacy studies with mouse and human tumors
TLDR
After the examination of 81 different Cryptophycin analogs in tumor bearing animals, C-309 has emerged as superior to all others and is being considered as second-generation clinical candidates. Expand
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