Anthracycline and anthraquinone anticancer agents: Current status and recent developments

Lown, J. William

doi:10.1016/0163-7258(93)90006-y

Cited by 153 publications

(29 citation statements)

References 52 publications

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“…Structurally, they are characterized by an anthraquinone‐based fused tetracyclic ring system, which is typically linked to an amino‐sugar. Since the discovery of daunorubicin in the early 1960s isolated from Streptomyces peucetius as the first anthracycline antibiotic with a marked anticancer activity in humans, a large number of natural, semisynthetic, and synthetic analogs have been evaluated for their biological and clinical properties . So far six members of this class are approved by the Food and Drug Administration (FDA), USA, for clinical use: daunorubicin, doxorubicin, epirubicin, idarubicin, and valrubicin (Fig.…”

Section: Anthraquinones As Drugsmentioning

confidence: 99%

“…At high drug concentrations, anthracyclines inhibit topoisomerase II activity by blocking access of the enzyme to DNA . Besides modulation of the activity of topoisomerases, other effects such as DNA intercalation, inhibition of DNA synthesis, induction of apoptosis, DNA unwinding, and free radical generation also may contribute to their antitumor activity …”

Section: Anthraquinones As Drugsmentioning

confidence: 99%

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Anthraquinones As Pharmacological Tools and Drugs

Malik

Müller

2016

Medicinal Research Reviews

336

211

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Anthraquinones (9,10-dioxoanthracenes) constitute an important class of natural and synthetic compounds with a wide range of applications. Besides their utilization as colorants, anthraquinone derivatives have been used since centuries for medical applications, for example, as laxatives and antimicrobial and antiinflammatory agents. Current therapeutic indications include constipation, arthritis, multiple sclerosis, and cancer. Moreover, biologically active anthraquinones derived from Reactive Blue 2 have been utilized as valuable tool compounds for biochemical and pharmacological studies. They may serve as lead structures for the development of future drugs. However, the presence of the quinone moiety in the structure of anthraquinones raises safety concerns, and anthraquinone laxatives have therefore been under critical reassessment. This review article provides an overview of the chemistry, biology, and toxicology of anthraquinones focusing on their application as drugs.

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Section: Anthraquinones As Drugsmentioning

confidence: 99%

Section: Anthraquinones As Drugsmentioning

confidence: 99%

Anthraquinones As Pharmacological Tools and Drugs

Malik

Müller

2016

Medicinal Research Reviews

336

211

View full text Add to dashboard Cite

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“…Doxorubicin (DOX)-based treatments are appropriate for many adult and pediatric solid tumors (including breast cancer), leukemias and lymphomas [1]. However, optimized administration of DOX is hampered owing to some toxicities, such as hematopoietic suppression, nausea, vomiting, and cardiotoxicity [2].…”

Section: Introductionmentioning

confidence: 99%

Association of ABCB1 and SLC22A16 Gene Polymorphisms with Incidence of Doxorubicin-Induced Febrile Neutropenia: A Survey of Iranian Breast Cancer Patients

et al. 2016

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Breast cancer is the most common cancer in women worldwide. Doxorubicin-based chemotherapy is used to treat breast cancer patients; however, neutropenia is a common hematologic side effect and can be life-threatening. The ABCB1 and SLC22A16 genes encode proteins that are essential for doxorubicin transport. In this study, we explored the effect of 2 common polymorphisms in ABCB1 (rs10276036 C/T) and SLC22A16 (rs12210538 A/G) on the development of grade 3/4 febrile neutropenia in Iranian breast cancer patients. Our results showed no significant association between these polymorphisms and grade 3/4 febrile neutropenia; however, allele C of ABCB1 (rs10276036 C/T) (p = 0.315, OR = 1.500, 95% CI = 0.679–3.312) and allele A of SLC22A16 (rs12210538 A/G) (p = 0.110, OR = 2.984, 95% CI = 0.743–11.988) tended to have a greater association with grade 3/4 febrile neutropenia, whereas allele T of ABCB1 (rs10276036) (p = 0.130, OR = 0.515, 95% CI = 0.217–1.223) and allele G of SLC22A16 (rs12210538) (p = 0.548, OR = 0.786, 95% CI = 0.358–1.726) tended to protect against this condition. In addition to breast cancer, a statistically significant association was also observed between the development of grade 3/4 febrile neutropenia and other clinical manifestations such as stage IIIC cancer (p = 0.037) and other diseases (p = 0.026). Our results indicate that evaluation of the risk of grade 3/4 neutropenia development and consideration of molecular and clinical findings may be of value when screening for high-risk breast cancer patients.

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“…The anticancer drug doxorubicin (DOX) is potent and therapeutically efficient for treatment of a variety of tumors [1,2]. However, it has considerable toxicity, which limits its therapeutic use, preventing treatment at high dosages, and it has an acquired resistance [3–6] excluding repeated treatment at tolerated dosages.…”

Section: Introductionmentioning

confidence: 99%

Cellular Delivery of Doxorubicin via pH-Controlled Hydrazone Linkage Using Multifunctional Nano Vehicle Based on Poly(β-L-Malic Acid)

Patil

Portilla-Arias

Ding

et al. 2012

IJMS

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Doxorubicin (DOX) is currently used in cancer chemotherapy to treat many tumors and shows improved delivery, reduced toxicity and higher treatment efficacy when being part of nanoscale delivery systems. However, a major drawback remains its toxicity to healthy tissue and the development of multi-drug resistance during prolonged treatment. This is why in our work we aimed to improve DOX delivery and reduce the toxicity by chemical conjugation with a new nanoplatform based on polymalic acid. For delivery into recipient cancer cells, DOX was conjugated via pH-sensitive hydrazone linkage along with polyethylene glycol (PEG) to a biodegradable, non-toxic and non-immunogenic nanoconjugate platform: poly(β-l-malic acid) (PMLA). DOX-nanoconjugates were found stable under physiological conditions and shown to successfully inhibit in vitro cancer cell growth of several invasive breast carcinoma cell lines such as MDA-MB-231 and MDA-MB- 468 and of primary glioma cell lines such as U87MG and U251.

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Anthracycline and anthraquinone anticancer agents: Current status and recent developments

Cited by 153 publications

References 52 publications

Anthraquinones As Pharmacological Tools and Drugs

Anthraquinones As Pharmacological Tools and Drugs

Association of ABCB1 and SLC22A16 Gene Polymorphisms with Incidence of Doxorubicin-Induced Febrile Neutropenia: A Survey of Iranian Breast Cancer Patients

Cellular Delivery of Doxorubicin via pH-Controlled Hydrazone Linkage Using Multifunctional Nano Vehicle Based on Poly(β-L-Malic Acid)

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