Over the last years, new agents have been introduced for the treatment of metastatic colorectal
cancer, the main objective being to prolong patient survival. One of these agents is bevacizumab
(Avastin; Genetech Inc.), a monoclonal antibody, a diffusible endothelial-specific mitogen and
an antibody to vascular endothelial growth factor (VEGF). VEGF is a secreted ligand that binds
to specific receptors expressed by angioblasts and endothe- lial cells [1] . The VEGF receptor
(VEGFR) family ligands, VEGF-1 and VEGF-2, are biologically related to angio- genesis …

 

 

Abstract Each year, about 5–6 cases out of 100,000 people are diagnosed with primary
malignant brain tumors, of which about 80% are malignant gliomas (MGs). Glioblastoma
multiforme (GBM) accounts for more than half of MG cases. They are associated with high
morbidity and mortality. Despite current multimodality treatment efforts including maximal
surgical resection if feasible, followed by a combination of radiotherapy and/or
chemotherapy, the median survival is short: only about 15 months. A deeper …

 

 

Importance of the field: Among various human CYPs, CYP2E1 is of particular interest
because of its involvement in the metabolic activation of many low molecular mass
procarcinogens. CYP2E1 induction, which may be a consequence of genetic polymorphism
or/and gene induction by xenobiotics, is the first step leading to the development of certain
chemically-mediated cancers. The aim of this review is to outline the current knowledge on
chemically-induced cancers through activation by CYP2E1, with emphasis on the …

 

Summary The sensitivity of breast neoplasms to hormonal control provides the basis of
novel investigational treatments with steroidal alkylators. An androsterone D-lactam
steroidal ester, the 3β-hydroxy-13α-amino-13, 17-seco-5α-androstan-17-oic-13, 17-lactam,
p-bis (2-chloroethyl) amino phenyl acetate (lactandrate) was synthesized and tested for
antitumor activity against six human breast cancer cell lines in vitro and against two murine
and one xenograft mammary tumors in vivo. A docking study on the binding interactions …

 

We tested two alkylating homo-aza-steroid esters, lactandrate and lactestoxate, for
antineoplastic activity against colon adenocarcinoma in vitro and in vivo. Cytostatic and
cytotoxic activity was evaluated in vitro with the SRB colormetric assay against nine human
colon adenocarcinoma cell lines. The in vivo anti-tumour effect was determined against two
rodent colon carcinomas, the Colon 26 and the relatively chemoresistant Colon 38
carcinoma, as well as against the human xenograft CX-1 colon carcinoma. Both of the …

In order to reduce toxicity and to increase antineoplastic activity, steroid molecules were
utilized as biological vectors for chemotherapeutic agents. Several modified steroid
compounds as 17ß-acetamido and D-homo-aza steroids that contain the NHCO group
outside or inside D steroid ring, respectively, were used in the synthesis of steroidal esters
carrying alkylating moieties. As it has been reported previously, several of these compounds
produced important both antileukemic and antitumor results. In this work, we …

Abstract Purpose This phase II study investigates the efficacy and safety of DNA
topoisomerase I inhibitor irinotecan plus bevacizumab a monoclonal antibody against VEGF
(BEVIRI) in patients with relapsed chemo-resistant SCLC. Methods Patients who previously
completed treatment with cisplatin–etoposide who relapsed within 3 months, had
measurable extensive-stage SCLC, ECOG performance status 0–2 and adequate
hematologic, renal and hepatic function, were given intravenous irinotecan 175 mg/m 2 …

Abstract Evidence indicating that hybrid steroid compounds of anti-cancer agents produce
reduced toxicity, significantly lower than the cytotoxic components alone, and increased anti-
cancer activity has prompted the design and development of such steroids, mostly alkylating
esters. We investigated the in-vitro and in-vivo activity of a homo-aza-steroidal alkylating
ester (HASE), in comparison with dacarbazine (DTIC), cisplatin (CPDD), carmustine (BCNU)
and semustine (MeCCNU), in the treatment of malignant melanoma. Cytotoxicity was …